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PharmQ2_Test1
| Question | Answer |
|---|---|
| This nervous system uses ACh as their signaling molecule | PNS(cholinergic) |
| This nervous system is thoracic/lumbar allowing for coordination | SNS (adrenergic) |
| This nervous system is craniosacral | PNS(cholinergic) |
| This nervous system releases DA, Epi & ACh | SNS (adrenergic) |
| ALL pre-ganglionic fibers in the PNS and SNS system release what? | ACh |
| Long post-ganglionic fibers in the PNS release what? | ACh |
| Long post-ganglionic fibers in the SNS release what? | NE; unlike in PNS which releases ACh(cholinergic) |
| Innervation to sweat glands mediated by: | ACh (SNS,adrenergic) |
| Innervation to adrenal medulla mediated by: | ACh |
| Somatic nn to skeletal mm (motor neuron) mediated by: | ACh |
| What's the ONLY post-ganglionic sympathetic fiber NOT using NE? | Sweat glands which use ACh |
| What does the adrenal medulla release? | NE and Epi |
| Dopamine is used to transmit to what? | Renal vasculature |
| Choline is synthesized to ACh via which enzyme? | ChAT |
| What INACTIVATES acetylcholine? | Acetylcholinesterase -Choline is then taken up into terminal |
| Tyrosine that enters the nerve terminal is converted to what? | DOPA then to dopamine |
| Tyrosine-->DOPA-->Dopamine is converted to what which will act on receptors? | Norepinephrine |
| Tyrosine is eventually converted into what nt? | Norepinephrine |
| This blocks DOPA synthesis | Metyrosine (blocks tyrosine) |
| This depletes NE in vesicle | Reserpine |
| This blocks re-uptake of NE | Cocaine, TCAs |
| This will function only in an INTACT terminal to increase NE release | Amphetamines, Tyramine |
| What metabolizes NE? | MAO & COMT |
| M1 receptors are found where? | Sweat glands & CNS |
| M1 receptors, found in sweat glands/CNS, release what? | DAG Gq/11 IP3 PLC |
| M2 receptors are found where? | Heart, smooth m, presynaptic |
| M2 receptors, found in heart, smooth m, presynaptic do what? | Gi Inhibit Adenylyl Cyclase |
| M3 receptors are found where? | Exocrine, smooth m, endothelium |
| M3 receptors found in exocrine, smooth m, endothelium activate what? | DAG Gq/11 IP3 PLC |
| These two receptor types activate DAG, Gq/11, IP3, PLC | M1 & M3 |
| This receptor is a Na+ channel for Nn & Nm | Nicotinic Receptor |
| This receptor is found in smooth m & excitatory | Alpha 1 |
| Alpha 1 receptors, found in smooth m & excitatory, activate what? | DAG Gq IP3 PLC |
| This receptor is found in PREsynaptic n terminals and some smooth m | Alpha 2 |
| Alpha 2 receptors, found in presynaptic n terminals & some smooth m activates what? | Gi INHIBITS adenylate cyclase |
| ALL Beta Receptors do what? | Stimulate Adenylate Cyclase (Gs) |
| Which Beta receptor increase rate and force of heartbeat? | Beta 1 |
| Which Beta receptor is present in bronchioles, heart, smooth m in skeletal blood vessel? | Beta 2 |
| What beta receptor is for lipolysis in fat cells? | Beta 3 |
| These dopamine receptors are present in the brain & vascular bed. INC cAMP | D1,D5 |
| These dopamine receptors are present in brain and other tissues. DEC cAMP | D2-4 |
| Repetitive stimulation would do what to the receptors? | Change Affinity or Down-Regulate |
| Lack of stimulation would do what to the receptors | Cause Affinity to INC or Up-Regulate |
| Which system is responsible for slowed gastrics & saliva? | PNS(cholinergic) |
| Which system causes sphincters to relax | PNS(cholinergic) |
| Which system causes pupils to constrict & accomodate for near vision | PNS(cholinergic) |
| Which system causes blood vessels to mm to dilate | SNS (adrenergic) |
| Which system causes bronchioles to dilate | SNS (adrenergic) |
| Which system causes pupils to dilate & inc distance vision | SNS (adrenergic) |
| Which system causes blood sugar, lipolysis to increase | SNS (adrenergic) |
| Which system causes renin to increase | SNS (adrenergic) |
| Which receptors would DEC heart rate & conduction? | M2 (PNS/cholinergic) |
| Which receptors cause bronchoCONSTRICTION | M3 (PNS/cholinergic) |
| Which receptors would INC heart rate, AV conduction, contraction | Beta 1/2 (SNS/adrenergic) |
| Which receptors would relax bronchioles | Beta 2 (SNS/adrenergic) |
| Which receptors would constrict MOST blood vessels | Alpha 1 (SNS/adrenergic) |
| Which receptor would relax some blood vessels | Beta 2 (SNS/adrenergic) |
| Which receptor would INC saliva & lacrimal secretion | M3 (PNS/cholinergic) |
| Which receptor would cause miosis & near vision accomodation | M3(PNS/cholinergic) |
| Which receptor would cause sweating | M1(PNS/cholinergic) |
| Which receptor would cause increase saliva | Alpha(SNS/adrenergic) |
| Which receptor would cause mydriasis | Alpha(SNS/adrenergic) |
| Which receptor would cause nasal vasoconstriction | Alpha(SNS/adrenergic) |
| Which receptor would stimulate GI contraction, relaxing sphincters | M3(PNS/cholinergic) |
| Which receptor would INC gastric acid secretion | M3(PNS/cholinergic) |
| Which two difft types of receptors would relax the GI tract | Alpha2 and Beta2 (SNS/adrenergic) |
| Which receptor would INC glyogenolysis in the liver | Beta2 (SNS/adrenergic) |
| In this system BOTH SNS and PNS work together | Genitourinary |
| Which receptor would contract bladder wall & release sphincters | M3 (PNS/cholinergic) |
| Which receptor promotes erection | M3(PNS/cholinergic) |
| Which receptor increases renin secretion | Beta1 (SNS/adrenergic) |
| Which receptor relaxes the bladder wall/uterus | Beta2 (SNS/adrenergic) |
| Which receptor contracts sphincters for ejaculation | Alpha1 (SNS/adrenergic) |
| Alpha receptors cause vasoconstriction and beta1 INC HR & contractility when this is released during the baroreceptor reflex | NE |
| Baroreceptors which detect increased pressure will activate the vagus n via ACh to do what? | DEC Heart Rate |
| Contraction of the iris circular m causes what? | Miosis (pupil constriction) -Contract via Muscarinic (PNS/Ach/Cholinergic) stimulation |
| Contraction of this eye m shifts lens & causes accomodation for NEAR vision. Also increases outflow of aqueous humor into canal of Schlemm | Ciliary m -Contract via Muscarinic (PNS/Ach/Cholinergic) stimulation |
| Stimulation of M receptors in the eye will not only cause miosis(pupil constrict) & accomodation, but what? | DEC intraocular pressure |
| Which receptors contract radial m leading to mydriasis (without cycloplegia) and DEC intraocular pressure | Alpha receptors (SNS, adrenergic) |
| Which receptors increase production of aqueous humor & INC intraocular pressure | Beta receptors (SNS, adrenergic) |
| Alpha blockers may cause this side-effect | Mydriasis (dilated pupils) |
| Beta blockers may cause this side-effect | Decreased secretion of aqueous humor therefore can use to treat glaucoma |
| M3 receptors are primarily responsible for PNS stimulation. What are the 2 exceptions where M2 take over? | Decrease SA node OR Decrease Atria Contraction |
| M3 receptors are primarily responsible for PNS stimulation. What is the 1 exception where M take over? (PNS only) | Penis, seminal vesicles (erection) |
| M receptors are present in both PNS/SNS. Where do you see it in SNS activation | Eccrine Sweat Glands |
| M receptors are present in both PNS/SNS. Where do you see it in PNS activation | Penis, seminal vesicles (erection) |
| What receptor is present primarily in the iris for SNS? | Alpha1 (SNS,adrenergic) |
| What receptor is present primarily in the heart for SNS? | Beta2(SNS,adrenergic) |
| Splanchnic skin vessels are innervated by what receptor | Alpha(SNS,adrenergic) |
| Skeletal m vessels are innervated by what receptor | Beta2(SNS,adrenergic) |
| Ejaculation of the penis (SNS) is caused by which receptor | Alpha(SNS,adrenergic) |
| This liver is primarily innervated by which receptor | Beta2(SNS,adrenergic) |
| Fat cells are primarily innervated by which receptor | Beta3(SNS,adrenergic) |
| Kidney is primarily innervated by which receptor | Beta1(SNS,adrenergic) |
| Metabolic functions and cardiac functions are controlled by which receptor for SNS activity | Beta (SNS,adrenergic) |
| Inhibits transporter which uptakes choline back into terminal | Hemicholinium |
| Inhibits release of ACh | Botulinum Toxin |
| Gq protein interaction-->PLC-->IP3 & DAG-->increase Ca2+-->Excitatory | M1,M3 receptors |
| When activated inhibit adenylate cyclase & are inhibitory | M2 |
| Respond to nicotine & are in brain, adrenal medulla, autonomic ganglia & NMJ. Receptor changes in response to blocking drugs in NMJ and autonomic ganglia. Is excitatory ion channel w/rapid desensitization | Nicotinic Receptors |
| When muscarinic agonists stimulate muscarinic receptors | Direct-acting |
| Cholinesterase inhibitors DEC breakdown of ACh and increase its duration in the cleft. Stimulates both muscarinic & nicotinic receptors | Indirect-Acting |
| ACh | Direct Agonist PNS _Act at both M and N receptors _Readily hydrolyzed by AChE |
| Methacholine | Direct Agonist PNS _Resistant to AChE _Act at both M and N receptors |
| Carbachol | Direct Agonist PNS _Resistant to AChE _Act at both M and N receptors |
| Bethanechol: Esters, Quartenary NH3 (does NOT enter CNS), poorly absorbed & not effective orally | Direct Agonist PNS _Resistant to AChE _Selective,does NOT enter brain |
| Pilocarpine | Direct Agonist PNS _Alkaloids _Selective for M receptor _Absorbed easily |
| Nicotine | Direct Agonist PNS |
| Sweat, salivary glands very sensitive to this | Pilocarpine |
| Selective for M3 receptors | Cevimeline |
| Found in some mushrooms | Muscarine |
| Responsible for PNS | Muscarinic Receptors |
| Can be used topically for glaucoma tx but will cause blurred vision because of it's affect on accomodation | Pilocarpine (a Muscarinic agonist) |
| Vagal stimulation by ACh causes atrial: bradycardia or tachycardia? | Bradycardia by slowing conduction through AV node |
| In the heart presynaptic M2 receptors affect NE how? | Decrease NE release and can no longer stimulate heart through beta receptors-->Bradycardia |
| Blood vesels (no cholinergic innervation) do have this receptor which through NO stimulation can cause vasodilation | M3 receptors |
| Do muscarinic agonists work often in the heart? | Used clinically for very FEW cardio effects |
| Increasing ACh will do what to the heart? | Bradycardia thru pre-synaptic upregulation of NE and vagal stimulation |
| Endothelial derived relaxing factor also known as | NO. Slows heart |
| M receptors cause this in the lungs | Bronchoconstriction: can be intense in asthmatics & vital capacity can be reduced. INC bronchial secretions |
| Used as a challenge to dx asthma patients | Methacholine (uses M receptors) |
| M receptors cause this in GI tract | INC motility and peristalsis INC tone INC salivary, gastric secretions Sphincters RELAX |
| Which muscarinic agonist has MOST GI effect | Bethanecol |
| M receptors cause this in urinary bladder | INC tone/peristalsis INC void pressure DEC bladder capacity Detrusor CONTRACTS Trigone & sphincter RELAX |
| Which muscarinic agonist has MOST Bladder effect | Bethanecol |
| M receptors cause this in the glands | INC secretion: sweat, lacrimal, nasopharyngeal, tracheobronchial |
| Which muscarinic agonist has MOST Sweat gland effect? | Pilocarpine (NOT Bethanecol) |
| These betel nuts are made of arecoline and cause this side effect | INC drooling/sweeating |
| Improves memory, alert, arousal & are used for Alzheimer's tx | Muscarinic agonists |
| What is most commonly used to INC GI motility after operative abdominal distension or gastric atony | Bethanechol (Urecholine) |
| Used to treat urinary retention, inadequate emptying. Post-op or post-partum or chronic myogenic or hypotonic bladder. | Bethanechol (Urecholine) |
| Can increase detrusor muscle contraction in patients with spinal cord injury | Bethanechol (Urecholine) |
| Dz dry mouth because of Sjogrens or head/neck radiation | Xerostomia |
| Used with most effect on salivation, though sweating is a common side effect. For Xerostomia Dx. | Pilocarpine |
| Selective M3 agonist that's long-lasting action w/few side effects. Shouldn't cause as much sweating as pilocarpine when treating Xerostomia. | Cevimeline (Evoxac) |
| Salivation, tears, nausea, vomting, diarrhea, headache, visual disturbances, bronchospasm & bradycardia/shock could also be caused by toxicity to this | Mushroom poisoning: muscarine |
| If pt is experiencing toxicity from muscarinics what should you treat with? | Atropine (antagonist) & albuterol to reverse the bronchoconstriction |
| Why is asthma/COPD contraindicated for muscarinics | Bronchoconstriction |
| Why is peptic ulcer contraindicated for muscarinics | INC GI acid |
| Why is bowel obstruction contraindicated for muscarinics | INC peristalsis |
| Why is coronary insufficiency contraindicated for muscarinics | May worsen cardiac problems |
| Responds to nicotine in autonomics, skeletal m & brain. Has 5 subunits. Ligand gated Na+ channel | Nicotinic receptors |
| Alfred has dry mouth, which would you prescribe with least side-effects? | Cevimeline |
| Nicotinic receptors in the brain when receive low doses of nicotine | INC alertness & attention |
| Muscarinic receptors do what in the eye | Constrict pupil, make more round w/ligaments relaxing |
| Nicotinic receptors in the brain when receive high doses of nicotine | Tremor, emesis, INC respiration |
| Nicotinic receptors in the brain when receive toxic doses of nicotine | Convulsions |
| Nicotinic receptors in gangion activate this nervous system | BOTH SNS and PNS |
| Sympathetic affects of nicotinic stimulation in ganglion | HTN Tachycardia, alternate w/vagal bradycardia |
| Parasympathetic affects of nicotinic stimulation in ganglion | Nausea, vomiting, diarrhea, urination |
| MUST be given IV infusion to slow heart and decrease BP | Acetylcholine |
| When these are desensitized there is muscle twitch or contraction followed by depolarizing block, paralysis in the NMJ | Nicotinic receptors |
| Vomiting, CNS stimulation(convulsions, coma, respiratory arrest), skeletal m depolarization (NMJ block & paralysis), cardiovascular (HTN, cardiac arrhythmia) caused by toxicity of this | Nicotine |
| Convulsions, coma & respiratory arrest are CNS toxicities for this | Nicotine |
| NMJ block & paralysis are skeletal mucle depolarization toxicities for this | Nicotine |
| HTN, cardiac arrhythmia are cardiovascular toxicities for this | Nicotine |
| This can be used to treat nicotine toxicity by blocking muscarinic receptors and decreasing PNS effects | Atropine |
| This can be used to treat nicotine toxicity by decreasing seizures | Anticonvulsants |
| This can be used to treat nicotine toxicity until nicotine induced paralysis of respiratory muscles is reversed | Respiration |
| This partial agonist on nicotinic receptor subtype in brain will prevent nicotine craving & nicotinic effect when pt does smoke | Chantix |
| Side effects of Chantix | Sleep, Flatulence Nausea, vomiting, sleep, constipation |
| "stigmines" (Neostigmine & Physostigmine) along w/Tensilon & Organophosphates (DFP, echothiophate, soman, sarin, parathion, malathion) are all examples of | Cholinesterase Inhibitors _INC time of ACh in cleft to activate receptors in cleft |
| Organophosphates which are used as a cholinesterase inhibitor | DFP, echothiophate, soman, sarin, parathion, malathion |
| "stigmine"s are example of this drug type which inhibits cholinesterase activity because they covalently bond & are hydrolyzed slowly by AChE | Carbamates |
| Carbamate that enters CNS. Used in eye. | Physostigmine (tertiary) |
| Carbamate that does NOT enter CNS. Poor oral absorption | Neostigmine (quartenary) |
| Reversible, short acting cholinesterase inhibitor. MUST be injected. Does NOT enter CNS | Edrophonium |
| Long-lasting effect that phosphorylates AChE and becomes irreversible with enzyme "aging". Functions as cholinesterase inhibitor | Organophosphates _lipid sol & released slowly for some time |
| This can be given to prevent aging or enzyme that would make organophosphates irreversibly effective. MUST be used within 3-4hrs | Pralidoxime (2-PAM) |
| Strong nucleophile, more effective at NMJ than at ganglia. Does NOT enter CNS. Can inhibit AChE & cause neuromuscular blockade so don't use unless indicated (usually w/organophosphates in 3-4hrs) | Pralidoxime (2-PAM) |
| AChE Inhibitor in CNS | Alertness, improve memory Convulsions & resp arrest w/poisoning |
| AChE Inhibitor in eye | Miosis, Near vision |
| AChE Inhibitor in GI, Bladder | stimulation, diarrhea, urination |
| AChE Inhibitor in respiration | salivation, secretion, bronchoconstriction |
| AChE Inhibitor in cardiovascular | ALL ganglia activated _PNS dominates -->Bradycardia, DEC contraction force, DEC cardiac output |
| Is there effect on blood pressure when you use AChE inhibitors | No cholinergic innervation therefore little effect on BP |
| Low concentrations of AChE Inhibiots at the NMJ | Intensify, prolong ACh action increasing muscular strength |
| What is used to treat myasthenia gravis? | AChE Inhibitors at low concentrations _Neostigmine (oral) |
| High concentrations of AChE Inhibiots at the NMJ | Twitches, fasiculations Neuromuscular blockade Paralysis at really high doses |
| Poorly orally used (but still used) lasts ~4hrs to increase bladder motility, reverse neuromuscular blockade in surgery & tx myasthenia gravis | Neostigmine (AChE Inhibitor) _May have some direct NMJ effect |
| Can be used to reverse neuromuscular blockade in surgery | Neostigmine (AChE Inhibitor) _May have some direct NMJ effect |
| Used in the tx of glaucoma, is rarely used orally bc can enter CNS and cause convulsions in high doses. May cause bradycardia. Effect ~2hrs | Physostigmine (AChE Inhibitor) |
| Used in the tx of atropine overdose, is rarely used orally bc can enter CNS and cause convulsions in high doses. May cause bradycardia. Effect ~2hrs | Physostigmine (AChE Inhibitor) |
| Donepezil, Rivastigmine, Galantamine, Tacrine are all what? | AChE inhibitors (lipid sol) _Enter CNS _Long Duration _Used tx Alzheimers |
| Used in the tx of alzheimers | AChE Inhibitors: Donepezil, Rivastigmine, Galantamine, Tacrine |
| Very short-acting used to dx myasthenia gravis: if myastenic, muscle strength will improve for ~5min(length of drug). | Tensilon |
| Very short-acting used to dx excessive AChE inhibitor tx: will decrease strength | Tensilon |
| Organophosphate AChE inhibitor: quartenary, not absorbed. Used in the eye to produce LONG lasting DEC in intraocular pressure in tx of glaucoma | Echothiophate |
| Organophosphate which irreversibly binds AChE inactivating it. Is a pesticide that's VERY lipid sol/volatile. Can be inhaled/absorbed thru skin/ingested. Gets into CNS & highly toxic | DFP (Diisopropylfluorophosphate) |
| Nerve gases (organophosphates) that are more potent, faster than DFP | Soman, Sarin, Tabun |
| Thiophosphate pesticide that's an organophosphate. Now OFF the market | Parathion |
| Thiophosphate pesticide that's an organophosphate. Inactivated by mammals so safer than other organophosphates | Malathion |
| To treat glaucoma want to more commonly use what? | A direct agonist: pilocarpine, carbachol |
| If you do not use a direct agonist to treat glaucoma what can you use? | Indirect agonist: Cholinesterase Inhibitor _Physostigmine, Echothiophate |
| What is one of the goals of treatments of glaucoma | Minimize systemic absorption |
| To treat closed-angle glaucoma until surgery is performed | Direct Agonist (Pilocarpine, Carbachol) +AChE Inhibitor |
| INC esophageal tone, gastric acid secretion/motility, intestinal motility (colon) is used to treat paralytic ileus. | Neostigmine (AChE Inhibitor) |
| INC esophageal tone, gastric acid secretion/motility, intestinal motility (colon) is used to treat atony of urinary bladder. | Neostigmine (AChE Inhibitor) _Bethanechol more commonly used |
| Treat atony of urinary bladder | Neostigmine (AChE Inhibitor) _Bethanechol more commonly used |
| Treat paralytic ileus | Neostigmine (AChE Inhibitor) |
| Autoimmune disease w/ab's to ACh receptors. See weak/fatigue & small head, neck extremity muscles | Myasthenia Gravis _Tx: AChE Inhibitor |
| Neostigmine, pyridostigmine & ambenonium can be used to increase the duration of action of ACh at the synapse(INC Receptor stimulation) for this disease | Myasthenia Gravis _Tx: AChE Inhibitor |
| During tx of Myasthenia Gravis with AChE Inhibitors muscarinic side effects & tolerance can occur. If too much drug is given pt's can become weak again. What do you use to determine whether the dose is right? | Edrophonium |
| Neuromuscular junction blockers are used in surgery to paralyze muscles, what can reverse the non-depolarizing block? | Cholinesterase Inhibitors like Neostigmine |
| SLUDGE is used to describe toxicity of AChE Inhibitors, what does it stand for? | Salivation, Lacrimation, Urination, Defecation, Gastric Distress, Emesis |
| Salivation, Lacrimation, Urination, Defecation, Gastric Distress, Emesis (SLUDGE) is toxicity caused by this | AChE Inhibitors |
| Besides SLUDGE, what other toxicities can occur because of AChE Inhibitors? | Miosis, sweating, bronchoconstriction, nausea, vomiting, diarrhea, bradycardia, HYPOtension CNS effects: confusion, ataxia, slurring, convulsions, coma |
| Neuromuscular stimulation followed by blockade leading to paralysis can happen upon this drug type administration | AChE Inhibitors |
| Pt has AChE Inhibitor poisoning caused by organophosphates. Tx? | Administer Atropine until pupils dilate (sign that it's overriding the inhibitor's pupillary contraction effects). If less than 3-4hrs since exposure give 2-PAM. Maintain respiration Give valium(Diazepam) for convulsions |
| Atropine does what to eyes? | Dilates pupils |
| Organophosphates (AChE Inhibitors) do what to pupils? | Constricts |
| What do AChE Inhibitors do to pupils? | Constricts _AChE; Organophosphates and "stigmines" and Tensilon |
| Sevin, Baygon and Temik can all cause symptoms of poisoning similar to organophosphates. What are they? | Carbamate AChE _Can use 2-PAM in these cases but controversial |
| Binds to muscarinic receptor but doesn't activate. Will displace ACh or agonists from receptor | Antimuscarinics(anticholinergic) _Atropine(Bella Donna): Dilates eye |
| Prodrug for antimuscarinic(anticholinergic) | Atropine: Used to dilate eye _Bella Donna _Enters CNS only at high doses |
| Antimuscarinic(anticholinergic) which enters CNS easily causing sedation, euphoria, amnesia. Can be used for motion sickness. | Scopolamine _Transdermal patch absorbed thru skin |
| Very short duration antimuscarinic(anticholinergic) used to dilate eye | Homatropine, tropicamide |
| Quarternary compound(therefore does NOT get in CNS) used to inhale for asthma, COPD. Antimuscarinic(anticholinergic) | Ipratropium, Tiotropium |
| Combined w/opiod for diarrhea | Atropine |
| Use for overactive bladder or after prostate surgery. Antimuscarinic(anticholinergic) | Tolterodine |
| Dose depends on prevailing tone of tissue w/effect on saliva, sweat glands, bronchiholes at low doses | Atropine |
| Atropine dose depends on prevailing tone of tissue w/effect on GI, urinary tract at what dose | High doses |
| Atropine dose depends on prevailing tone of tissue w/effect on CNS at what dose | High doses _CNS stimulation followed by depression; can cause confusion & coma |
| Dry mouth side-effect of these type of drugs | Antimuscarinic(Anticholinergic) |
| Drowsiness, memory loss. Used to relieve motion sickness. Dries up secretions, pre-anesthesia. | Scopolamine _Antimuscarinic(Anticholinergic) |
| Toxic side effect: hallucination, agitation, coma | Scopolamine _Antimuscarinic(Anticholinergic) |
| Blocks iris sphincter, pupil dilates, can't focus(inhibited ciliary m), photophobia. _Narrow Angle Glaucoma contraindicated _Dry Eyes | Tropicamide _Antimuscarinic(Anticholinergic) |
| Order of eye effect on Antimuscarinic(Anticholinergic) drugs length | Atropine>Scopolamine>Homatropine>Cyclopentolate>Tropicamide |
| Stimulate M2 receptors in atria & SA node. Presynaptic M2 receptors decrease NE release & HR decrease | Muscarinic(Cholinergic) |
| Effect of Antimuscarinic(Anticholinergic) on heart | Tachycardia due to DEC in vagal tone since M2 receptors are blocked. _NE release INC bc of presynaptic M2 block |
| Do Antimuscarinic(Anticholinergic) have effect on heart ventricles? | Little effect |
| Do Antimuscarinic(Anticholinergic) have effect on babies or elderly? | Very little effect because there is small vagal tone in these patients |
| Do Antimuscarinic(Anticholinergic) have effect on blood vessels? | Little effect, but can block vasodilation caused by NO in response to muscarinic agonists. |
| Useful for muscarinic poisoning because can block vasodilation caused by NO release | Antimuscarinic(Anticholinergic) |
| In overdose can cause vasodilation in the face(to decrease heat) | Atropine: Antimuscarinic(Anticholinergic) |
| Blurred vision | Side effect of Antimuscarinic(Anticholinergic) |
| Dry eyes | Side effect of Antimuscarinic(Anticholinergic) |
| Dry mouth | Side effect of Antimuscarinic(Anticholinergic) |
| Can reverse bronchoconstriction or cause dilation. Useful for ACUTE asthma attacks & COPD | Antimuscarinic(Anticholinergic) _Ipratropium(inhaled for local effects) _Tiotropium(inhaled for local effects) |
| Antimuscarinic(Anticholinergic) that decreases secretions in respiratory & causes sedation. Was once given before inhalation anesthesia | Scopolamine |
| DEC motility & secretions in GI tract. Antispasmodic, reduces tone & propulsion. | Antimuscarinic(Anticholinergic) |
| Combined w/opioid(diphenoxylate)to treat diarrhea...called Lomotil | Atropine _Antimuscarinic(Anticholinergic) |
| DEC motility in bladder. Used to tx overactive bladder but may cause urinary retention in men w/benign prostatic hyperplasia | Antimuscarinic(Anticholinergic) _Tolterodine _Darifenacin, solifenacin _Oxybutynin, trospium |
| Used to treat overactive bladder, selective M3 with no CNS effect | Tolterodine (Antimuscarinic(Anticholinergic)) _Beware: can cause urinary retention in men w/benign prostatic hyperplasia |
| Prevent bladder spasm after prostate surgery | Oxybutynin, Trospium (Antimuscarinic(Anticholinergic)) _Beware: can cause urinary retention in men w/benign prostatic hyperplasia |
| Inhibition of sweat & lacrimal glands. Body temp increases w/toxic doses (esp children). Decreased salivation even at low doses. Dry mouth frequent. | Antimuscarinic(Anticholinergic) |
| Dilate eye(mydriasis) & produces cycloplegia. Administer directly in eye, want short acting. | Antimuscarinic(Anticholinergic) |
| Side effects on eye include photophobia, increased ocular pressure in glaucoma | Antimuscarinic(Anticholinergic) |
| Used as antispasmodic in GI tract | Dicylomine _Antimuscarinic(Anticholinergic) |
| Decreases GI side effects from AChE inhibitors in Myasthenia Gravis | Antimuscarinic(Anticholinergic) |
| Used to DEC bradycardia(by reversing excess vagal stimulation and/or reversing heart block). Used after MI | Atropine _Antimuscarinic(Anticholinergic) _Causes tachycardia(INC HR) |
| Used in surgery to prevent excess vagal reflexes | Glycopyrrolate _Antimuscarinic(Anticholinergic) |
| Used in lung to reverse cholinergic stimulation that causes bronchospasm. Use for COPD and ACUTE asthma | Tiotropium(Spiriva) Antimuscarinic(Anticholinergic) |
| M3 antagonists used for urinary incontinence. Side effects: dry mouth, blurred vision | Tolterodine (Detrol) _Toviaz, Enablex,Vesicare _Antimuscarinic(Anticholinergic) |
| Usually bladder spasms occur after prostate surgery, blocking muscarinic receptors would dec bladder tone/spasm. Use? | Oxybutynin(Ditropan) _Antimuscarinic(Anticholinergic) _Dry Mouth |
| Used as adjunct therapy when DA replacement not enough in Parkinson's. | Antimuscarinic(Anticholinergic) |
| Reverses extrapyramidal effects of antipsychotics | Antimuscarinic(Anticholinergic) |
| Dry mouth, decreased bronchial secretions, tahcycardia, mydriasis(pupil dilation), cycloplegia, DEC GI motility, urinary retention, dry skin/decreased sweating | Side effects of Antimuscarinic(Anticholinergic) |
| Narrow angle glaucoma will be contraindicated for these drugs bc the drugs will INC intraocular P & aqueous humor has nowhere to go | Antimuscarinic(Anticholinergic) |
| Benign prostate hyperplasia contraindication for this since increases difficulty urinating | Antimuscarinic(Anticholinergic) |
| Dry as a bone, blind as a bat, red as a beet, mad as a hatter | Antimuscarinic(Anticholinergic) Overdose _Atropine overdose |
| Constipated, urinary retention, poor vision, delirium, cardio/resp collapse | Antimuscarinic(Anticholinergic) Overdose |
| Antihistamine(Benadryl) | Antimuscarinic(Anticholinergic) effects |
| Tricyclic antidepressants | Antimuscarinic(Anticholinergic) effects |
| Antipsychotics | Antimuscarinic(Anticholinergic) effects |
| Eyedrops | Antimuscarinic(Anticholinergic) effects |
| Anti-diarrhea preparations | Antimuscarinic(Anticholinergic) effects |
| Who is most effected by Antimuscarinic(Anticholinergic) overdose? | Children |
| If have pesticide or nerve gas poisoning what should you use to block muscarinic effects | Atropine _Antimuscarinic(Anticholinergic) _Inject until pupils dilate & mouth is dry. Keep injecting till poison wears off |
| If have mushroom poisoning what should you use to block muscarinic effects | Atropine _Antimuscarinic(Anticholinergic) _Inject until pupils dilate & mouth is dry. Keep injecting till poison wears off |
| How would you block neuromuscular? | Block nicotinic receptor on skeletal m. |
| Stimulate before blockade of neuromuscular | Depolarizing neuromuscular blocker(Anti-nicotinic) |
| Competetive antagonists that produce direct blockade of neuromuscular | Non-depolarizing neuromuscular blocker(Anti-nicotinic) _Tubocurarine |
| Used to produce paralysis in surgery | Neuromuscular blocker |
| Binds top gate of NMJ Nicotinic receptor which allows Na+ influx and contraction | Succinylcholine |
| Blocks receptor preventing effect of ACh, inhibiting m contraction. Competetive/Reversible. Used in surgery to relax muscle | AChE inhibitors_Nondepolarizing block _Will reverse INC amt of ACh & compete for receptor |
| Highly ionized (No CNS effects, must be given IV). 1-6mins onset. Causes motor weakness, small muscles effected first | Non-Depolarizing Drugs(anti-nicotinic) |
| With non-depolarizing drugs(anti-nicotinic), what is the last muscles to be effected | Respiratory muscles |
| Depolarizes BEFORE blocking NMJ, therefore there's an initial contraction before paralysis. Has very brief action w/rapid onset | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Transient m fasciculations, paralyze arm/neck/leg/face/pharynx/respiratory mm. Onset ~1min. Lasts 5-10 mins unless cholinesterase abnormal. | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Metabolized by plasma pseudocholinesterase. Genetic variation determines duration of action. Has initial contraction followed by brief spastic paralysis. | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Possible side-effect of succinylcholine tx since this is released when nicotinic receptors are stimulated. Common w/denervated m or burns. | INC K+ causes Hyperkalemia _Can cause Cardiac Arrest |
| Side-effect includes post-op muscle pain due to initial fasciculations | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Side-effect includes INC intragastric pressure, emesis during initial fasciculations | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Side-effect of this anti-nicotinic includes INC intraocular pressure. | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| Side-effect includes Malignant Hyperthermia | Halothane _Depolarizing Drugs(anti-nicotinic) |
| Contraindicated if: extensive soft tissue damage severe burns nontraumatic rhabdomylosis Quadriplegia, Paraplegia Muscular Dystrophy In children <8 y/o | Succinylcholine _Depolarizing Drugs(anti-nicotinic) |
| NMJ block (anti-nicotinics) can be enhanced by | Some inhaled anesthetics Local anasthetics Aminoglyocisde Abx Tetracyclines Ca2+ channel blockers |
| Aminoglycosides which depress evoke ACh release can be coupled w/what to enhance NMJ block | Anti-Nicotinic _ie succinylcholine |
| Tetracyclines, which chelate Ca2+, can be coupled w/what to enhance NMJ block | Anti-Nicotinic _ie succinylcholine |
| Ca2+ channel blockers can be coupled w/what to enhance NMJ block | Anti-Nicotinic _ie succinylcholine |
| Pt has myasthenia gravis, how would you use an anti-nicotinic (NMJ blocker)? | Cautious since NMJ function already poor |
| Pt is elderly, how would you use an anti-nicotinic (NMJ blocker)? | Decrease dose since there is decreased clearance of drug/longer action |
| Pt w/severe burns, UMN disease which is resistant to non-depolarizing blockers. What would happen if given Succinylcholine | Hyperkalemia since K+ builds up |
| Used in surgery, ventilation, orthopedics, intubation, ECT to prevent m spasms | Anti-Nicotinics _Depolarizing or Non-depolarizing |
| Blocks nicotine receptors at ALL autonomic ganglia. Non-depolarizing competitive antagonist that DEC total autonomics. Once used to tx HTN. | Ganglion Receptor Blockers _Anti-Nicotinic |
| Ganglion blockers: Used to cause cycloplegia, mild dilation of pupil | Ganglion Blockers: _Hexamethonium _Mecamylamine |
| Ganglion blockers: Used for SNS innervation, vasodilation, DEC BP, DEC vasomotor tone & orthostatic HYPOtension | Ganglion Blockers: _Hexamethonium _Mecamylamine |
| Ganglion blockers(Hexamethonium, Mecamylamine) in heart | Block contraction DEC vagal tone-->Tachycardia |
| Ganglion blockers(Hexamethonium, Mecamylamine) in GU | Bladder tone DEC Urinary retention w/BPH DEC ejection/erection |
| Ganglion blockers(Hexamethonium, Mecamylamine) in glands | Leads to no sweating (blocked autonomics) |
| Beta 2 receptors ONLY stimulated by this | Epinephrine |
| Stimulates alpha and Beta-1 | NE |
| Stimulates all alpha & beta receptors | NE |
| Inhibits tyrosine hydroxylase | Metyrosine |
| Cocaine/antidepressants inhibit this | Re-uptake of adrenergics(NE) |
| Metabolizes adrenergics(NE) | MAO |
| Constrict blood vessels to skin, kidney, mucous membrane | Alpha 1+Adrenergic stimulation |
| Relax blood vessels to skeletal m | Beta 2+NE (NOT Epi because Epi can't bind beta2) |
| Stimulate salivary, sweat glands | M receptor+Adrenergic Stimulation |
| Relax gut wall, bronchioles | Beta 2+NE (NOT Epi because Epi can't bind beta2) |
| Excites cardiac | Beta+Adrenergic Stimulation |
| Causes glycogenolysis, lipolysis | Beta+Adrenergic Stimulation |
| Modulates insulin, renin | Beta+Adrenergic Stimulation |
| Respiratory stimulation, awak, DEC appetite | +Adrenergic Stimulation |
| Inhibits transmitter release | Alpha2+Adrenergic Stimulation |
| Act on receptors to mimic SNS stimulation in noradrenergic terminal | Direct agonist |
| Increase synthesis, cause release or inhibit re-uptake/breakdown at the noradrenergic terminal | Indirect agonist _Cocaine, tyramine, amphetamine |
| Denervation will abolish the effect of what type of agonists? | Indirect agonist _Cocaine, tyramine, amphetamine |
| Denervation will enhance the effect of what type of agonists? | Direct agonist |
| Within alpha receptor which stimulates first: Epi, NE or Isoproterenol | Epinephrine will always bind MORE |
| Within alpha receptor which stimulates second: Epi, NE or Isoproterenol | NE will bind less than Epi but MORE than Isoproterenol |
| Within alpha receptor which stimulates last: Epi, NE or Isoproterenol | Isoproterenol never binds as well |
| When alpha1 is stimulated by adrenergics what happens? Molecule? | Phenylepinephrine _EXCITES |
| When alpha2 is stimulated by adrenergics what happens? Molecule? | Clonidine _INHIBITORY _pre-synaptic |
| Vasoconstriction, INC peripheral resistance | Alpha1+Phenylepinephrine _Excitatory |
| Vasoconstriction in nasal mucosa | Alpha1+Phenylepinephrine _Excitatory |
| Mydriasis | Alpha1+Phenylepinephrine _Excitatory |
| Prostate, bladder base, urethral sphincter: contract & promote urinary continence | Alpha1+Phenylepinephrine _Excitatory |
| Intestinal smooth m relax | Alpha1+Phenylepinephrine _Excitatory |
| Stimulate pilomotor smooth m | Alpha1+Phenylepinephrine _Excitatory |
| Presynaptic, decrease NE release causing overall DECREASE in blood pressure | Alpha2+Clonidine _Inhibitory |
| Inhibit ACh release decreasing intestinal tone & secretion. Cause platelet aggregation, coronary/skin/mucosal/renal vasoconstriction, decrease insulin secretion | Alpha2+Clonidine _Inhibitory |
| Platelet aggregation | Alpha2+Clonidine _Inhibitory |
| Decrease insulin secretion | Alpha2+Clonidine _Inhibitory |
| MOST effective on beta receptors | Isoproterenol>Epinephrine/NE |
| B1 receptor effectiveness | Isoproterenol>Epinephrine=NE |
| B2 receptor effectiveness | Isoproterenol>Epinephrine>>NE |
| B3 receptor effectiveness. | Isoproterenol=NOREPInephrine >Epinephrine Only one where NE binds more than Epinephrine |
| Stimulation of this receptor is the ONLY one which has NE bind MORE than epinephrine | Beta3 |
| Stimulation of this receptors are ones where Epi binds more than NE | Beta2 |
| Stimulation of this receptor is equal for both Epi/NE. Still less than Isoproterenol | Beta1 |
| INC HR & force of contraction, automaticity, conduction AV node. INC renin secretion | Beta 1 receptors _Stimulant=Dobutamine |
| Relax bronchial smooth m, skeletal muscle blood vessels, uterus, bladder, GI muscle, glycogenolysis/gluconeogenesis, K+ uptake into skeletal m | Beta 2 receptors _Stimulant=Albuterol |
| INC glycogenolysis, gluconeogenisis | Beta 2 receptors _Stimulant=Albuterol |
| INC Na/K ATPase stimulating K+ uptake into skeletal m | Beta 2 receptors |
| Stimulate lipolysis in fat cells | Beta 3 receptors |
| Dobutamine stimulates this receptor | Beta 1. Effecting INC heart rate/conduction/contraction. INC renin secretion |
| Albuterol stimulates this receptor | Beta 2 to relax bronchial smooth m, skeletal m blood vessels. |
| Asthma patient who overuses albuterol(beta 2 agonist) if constantly uses meds what will happen | Beta2 receptors will down-regulate and drug dose will no longer be effective |
| Dilate renal blood vessels & INC renal blood flow. | Dopamine receptors stimulated by adrenergics |
| INC arterial resistance, effect greatest in small vessels(skin). Will INC blood pressure(stimulates baroreceptors. Activate Vagus, slows HR) | Alpha receptor stimulation by adrenergics |
| In atherosclerosis effects of these receptors may be increased while baroreceptors effect are decreased | Alpha receptor agonists _Adrenergic Stimulation |
| Contract radial pupillary dilator m (Mydriasis). NO effect on accommodation. Used to treat glaucoma. | Alpha receptor agonists _Adrenergic Stimulation |
| Constrict nasal & upper airway blood vessels. Used as decongestants | Alpha1 receptor agonist _Adrenergic Stimulation |
| Relax GI smooth m | Alpha1 receptor agonists _Adrenergic Stimulation |
| Inhibit ACh release in GI | Alpha2 receptor agonists _Adrenergic Stimulation |
| INC continence, constrict sphincter | Alpha1 receptor agonists _Adrenergic Stimulation |
| Needed for ejaculation | Alpha receptor agonists _Adrenergic Stimulation |
| Inhibits lipolysis, insulin secretion & decrease renin secretion | Alpha receptor agonists _Adrenergic Stimulation |
| INC force/rate of contraction in heart. Ca2+ influx INC. INC nodal conduction, DEC refractory period. INC contraction. | Beta receptor agonists _Adrenergic Stimulation |
| INC need for Oxygen consumption | Beta receptor agonists _Adrenergic Stimulation |
| Dilation of blood vessels in skeletal m, DEC diastolic BP | Beta2 receptor agonists _Adrenergic Stimulation |
| Increase INTRAOCULAR Pressure in eye | Beta receptor agonists _Adrenergic Stimulation |
| Relax uterus & bladder wall | Beta receptor agonists _Adrenergic Stimulation |
| Relax bronchial smooth m | Beta receptor agonists _Adrenergic Stimulation |
| INC renin secretion | Beta1 receptors _Adrenergic Stimulation |
| Stimulate glycogenolysis, INC K+ uptake into cell, increase insulin secretion | Beta2 receptors _Adrenergic Stimulation |
| Stimulate lipolysis | Beta3 receptors _Adrenergic Stimulation |
| Must be injected. INC periph Resistance, BP, DEC blood flow to kidney/spleen/liver, HR INC. No change to Cardiac Output | NE _Short-Action causing vasoCONSTRICTION @infusion site |
| If you give Atropine prior to NE what will happen? | Atropine will block vagal reflex by baroreceptors and HR will increase |
| Used to reverse HYPOtension. Injected. Will cause necrosis if poor blood flow because it causes so much vasoCONSTRICTION | Norepinephrine |
| INC Systolic BP & DEC diastolic BP. Pulse pressure INC, mean pressure doesn't change | Epinephrine |
| Cardiac output INC, oxygen consumption increase | Epinephrine |
| Low dose of epinephrine being give. What receptors are stimulated. | Beta-2 (more sensitive to epi than alpha) _VasoDILATION |
| High dose of epinephrine being give. What receptors are stimulated. | Alpha receptors (less sensitive to epi than beta therefore need larger dose) _VasoCONSTRICTION |
| Blood vessels are more sensitive to these receptors and thus a small dose of epinephrine will effect this first | Beta 2 _Alpha only stimulated at high dose because LESS sensitive |
| INC cardiac output, oxygen consumption. Blood glucose INC, glycogenolysis(b2), lipolysis(b3), renin INC, bronchodilation(b2). Short action, must be injected | Epinephrine |
| Reverses epinephrine effect | Alpha Block |
| Prevents HR increase | Beta Block |
| Used for severe asthma attack by causing bronchodilation | Epinephrine_beta2 |
| DEC diffusion of injected drugs(local anesthetics) | Epinephrine_VasoCONSTRICTION |
| Restore BP, bronchodilation, DEC angioedema, reverse cardiovascular collapse in Anaphylactic Shock | Epinephrine |
| Used for cardiac arrest & complete heart block | Epinephrine |
| Throbbing heeadache, palpitations, restlessness, tremor, worsened angina | Epinephrine |
| Rapid, large doses may cause cerebral hemorrhage due to HYPERtension | Epinephrine |
| Possible ventricular arrhythmia | Epinephrine side effect |
| If beta receptors are blocked what happens when inject epinephrine | INC blood pressure |
| Release NE, stimulates alpha/beta receptors w/similar effects to epinephrine. BronchoDILATOR, CNS stimulant. Used in weight loss drugs. Death from HI BP, stroke. | Ephedrine(Ephedra, Ma Huang) |
| VasoCONSTRICTION increasing periph vascular resistance. BP goes up, reflex slowing of heart. Use for HYPOtensive emergencies. Decongestant. Mydriasis(dilated pupil) seen. | Alpha agonists |
| Methyldopa | Alpha2 agonist used for HYPERtension |
| Apraclonidine | Alpha2 agonist used for glaucoma |
| Brimonidine | Alpha2 agonist used for glaucoma |
| Tizanidine | Alpha2 agonist used for m relaxant |
| Binds Beta(more than alpha) to INC heart rate/contract force via baroreceptor reflex. INC Cardiac Output. VasoDILATES skeletal m, renal vascular bed. DEC BP. | Isoproterenol (brief action) _ER tx of cardiac arrest, complete heart block _ER tx of asthma _Large Doses-->palpitation, tachycardia, arrhythmia |
| Selective b1 agonsit which INC heart contraction force. INC Card Output in shock & CHF. Has only a small effect on peripheral resistance & HR. | Dobutamine _Use for STRESS TESTS, Echo _If pt HTN, BP may increase too quickly |
| When administering dobutamine to a patient to test for stress test and pt is hypertensive what could happen? | BP may increase if given too quickly, therefore administer slowly |
| Used to relax uterus in premature labor. Main side effect: headache | Ritrodine _Beta2 agonist |
| Inhaled for asthma tx. Can see tremor, tachycardia, palpitations. Will see headaches if given systemically. | Albuterol _Beta2 agonist |
| Not albuterol, but used in asthma tx | Terbutaline, Pirbuterol, Bitolterol, Salmeterol |
| D1 agonist that vasoDILATES renal vascular beds. Tx for cardiac shock by INC blood flow & CO without vasoconstriction. | Dopamine |
| High doses of this will stimulate beta-1 receptors in heart and may increase the release of NE & INC BP | Dopamine _Usually D1 agonist used to vasodilate renal vascular beds & tx cardiac shock |
| SELECTIVE D1 agonist that dilates vascular beds. Used to DEC BP. | Fenoldopam |
| Causes release of NE indirectly (esp in brain). Peripherally causes HTN, tremor, tachycardia. CNS causes psychosis, alert, euphoria, insomnia, DEC appetite, INC motor activity | Amphetamine |
| Side effects of Amphetamine | Headache, dizziness, palpitations, agitation, confusion, DELIRIUM @High Doses: HTN, cerebral hemorrhage, convulsions or coma |
| Popular drug of abuse with more central actions (euphoria, insomnia, DEC appetite, psychosis, INC motor activity) | Methamphetamine |
| Decreases hyperactivity in ADHD | Ritalin (Methylphenidate) _Form of Amphetamine |
| Inhibits DA & NE re-uptake indirectly. Short acting, intense esp if smoked. Effects similar to amphetamine. Causes severe HTN, possible stroke. Tachycardia/arrhythmia possible. May cause psychosis. Used to decrease local blood flow/local anesthesia. | Cocaine _Should be used to DEC local blood flow & use for local anesthesia |
| Cocaine+Amphetamine would lead to what response? | Overall prolonged response |
| Indirectly INC NE release from terminals by displacing them from vesicle forming a false transmitter OCTOPAMINE. Repeated application causes TACHYPHYLAXIS. | Tyramine _Hydrolyzed by MAO before much absorbed _MAOI will cause massive NE release=SEVERE HTN |
| Beta2 receptors do what to insulin release? | INC insulin release |
| If MAO is blocked or tyramine is injected, what may occur? | Massive NE release-->SEVERE HTN |
| Decongestant which constricts nasal & upper resp blood vessels. Rebound effect possible. Systemically used may INC BP. | Phenylephrine: spray/oral _Pseudoephedrine(may be more effective) _Mydriasis occurs but DO NOT affect accomodation. Used as eye drops in retinal exam |
| Used as eye drops in retinal exam because causes mydriasis without affecting accomondation. | Phenylephrine/Pseudoephedrine |
| Direct acting alpha agonist used topically. Rebound effect can occur w/chronic use (receptor DOWNRegulation) | Topical Alpha Agonist "zolines" |
| Xylometazoline & Oxymetazoline | Topical Nasal Sprays "zolines" _Alpha Agonists |
| Tetrahydrozoline & Naphazoline | Used in eye to get red out "zolines" _Alpha Agonist _DO NOT use in Narrow Angle Glaucoma or HTN |
| Pt has narrow angle glaucoma & HTN can you use a topical ALPHA agonist? | NO. Not allowed to use any "zolines" |
| Selective alpha2 agonist (in brain will presynaptically inhibit NE release). Causes DEC in SNS output from CNS. DEC peripheral resistance, BP & HR | Clonidine (Catapres)-oral or patch _HTN tx _DEC craving in addicts _DEC hot flashes _Pre-Anesthesia |
| _HTN tx _DEC craving in addicts _DEC hot flashes _Pre-Anesthesia | Clonidine (Catapres)-oral or patch _Side Effects: dry mouth, sedation, sexual dysfunction, can exacerbate depression. _WILL cause SEVERE HTN if withdrawn too quickly |
| Do not withdraw Clonidine (Catapres) too quickly when tx for HTN/craving/hot flashes/pre-anesthesia. Why? | Will cause SEVERE HTN if withdrawn too quickly |
| Alpha2 agonists used for HTN tx | Guanbenz Guanfacine Methyldopa |
| Alpha2 agonists used for glaucoma | Apraclonidine Brimondine |
| *Which drugs is beta 1 selective and has ISA? | Acebutolol |
| Alpha2 agonists used for muscle relaxant | Tizanidine |
| Increases rate & force of contraction in heart. VasoDILATES skeletal m, renal vascular bed leading to decreased BP. The baroreceptor reflex will help to INC HR and decrease Cardiac Output. | Isoproterenol _INC HR & DEC BP _Brief action _Large doses may cause palpitation, tachycardia, arrhythmia |
| Used for ER tx of cardiac arrest, complete heart block, ER astham | Isoproterenol _INC HR & DEC BP _Brief action _Large doses may cause palpitation, tachycardia, arrhythmia |
| Selective beta-1 agonist that INC contraction force of heart. Little effect on peripheral resistance or HR. | Dobutamine _INC CO in shock and CHF _Used for STRESS test, Echo |
| Increases CO in shock and CHF | Dobutamine _Use for stress test, echo _Inc contraction force of heart |
| Used to relax uterus in premature labor. Beta 2 agonist | Ritrodine _Side effect: head ache |
| Inhaled for ashtma tx causes tachycardia, tremor, palpitations. | Albuterol _Headache common w/systemic administration |
| Terbutaline, pirbuterol, bitolterol, salmeterol used for tx of this. Are beta2 agonists | Asthma tx |
| D1 agonist used for vasoDILATION of renal vascular beds. Used to treat cardiac shock, INC blood flow & Cardiac Output without vasoconstriction. | Dopamine _High doses stimulate beta2 receptors in hear, may also INC NE release & INC BP |
| High doses stimulate beta2 receptors in hear, may also INC NE release & INC BP | Dopamine _D1 Agonist |
| Highly selective D1 agonist that dilates vascular beds. Used to DEC BP. | Fenoldopam |
| Causes release of NE indirectly in the brain causing tremors, tachycardia & HTN in periphery | Amphetamine _Ritalin is a form _Side effect: headache, dizziness, palpitations, agitation, confusion, delirium, HTN, cerebral hemorrhage, convulsions or coma |
| Causes release of NE indirectly in the brain causing alert, euphoria, insomnia, DEC appetite, INC motor activity, psychosis possibly | Amphetamine _Ritalin is a form _Side effect: headache, dizziness, palpitations, agitation, confusion, delirium, HTN, cerebral hemorrhage, convulsions or coma |
| At very high doses this drug which releases NE indirectly can cause HTN, cerebral hemorrhage, convulsions or coma | Amphetmaine |
| Methamphetamine | Popular drug of abuse w/more central actions |
| Methylphenidate (Ritalin) | DEC hyperactivity in ADHD |
| Inhibits DA & NE reuptake (indirectly). Short intense effect similar to amphetmaine. Can cause severe HTN, possible stroke, tachycardia, arrhythmia, psychosis. | Cocaine _Used to DEC local blood flow & for local anesthesia |
| Used to DEC local blood flow & for local anesthesia | Cocaine (inhibits reuptake of DA & NE) |
| Indirectly INC NE release from n terminals. Displaces NE from vesicle forming a false transmitter (octopamine) | Tyramine _Repeated application causes tachyphylaxis _Hydrolyzed by MAO before much absorbed |
| If MAO blocked or this drug is injected may cause massive NE release leading to severe HTN | Tyramine _Displaces NE from vesicle forming false transmitter & will indirectly INC NE release from n terminals. |
| If alpha receptors are blocked, which will dominate adrenergic effects | Beta receptors |
| If beta receptors are blocked, which will dominate adrenergic effects | Alpha receptors |
| Causes mydriasis, vasoCONSTRICTION, contractino of GU m, ejaculation | Alpha1 receptors |
| Decreases NE release & suppresses insulin secretion | Alpha2 receptors |
| Blockade will cause DEC peripheral vascular resistance, BP, venous return. Also causes Miosis, nasal congestion, improved urine flow, inhibit ejaculation, INC NE release | Alpha Blockade |
| When blocked causes miosis, nasal congestion | Alpha Blockade |
| Improves urine flow especially in men (relaxes base of bladder & prostate). Inhibits ejaculation | Alpha Blockade |
| INC HR/force of contraction & renin secretion | Beta1 receptor |
| Decreases HR/Force of contraction, Cardiac Output, Oxygen Demand, Renin secretion | Beta Blockade _This will DEC BP in pt's w/HTN and reduce INC in HR & BP in response to exercise or stress |
| Causes bronchoconstriction therefore be careful when patient is asthmatic & using this to treat for HTN | Beta Blockade |
| Causes DEC glycogenolysis, lipolysis, intraocular pressure | Beta blockade |
| Because beta blockers can decrease intraocular pressure what can you use it for | Glaucoma tx |
| Reversible alpha antagonist | Labetalol Phenotolamine Prasozin, Terasozin, Doxasozin Tamsulosin Tolazoline |
| Irreversible alpha antagonist | Dibenamine Phenyoxybenzamine |
| Will DEC vasoconstriction(aa & vv) & will lower peripheral vascular resistance especially when standing | Alpha Blockade |
| Causes reflex tachycardia: the DEC BP will stimulate baroreceptors & effect of increased NE will be on beta receptors. | Alpha Blockade _DEC Vagal Output |
| May allow INC NE release, again stimulating beta receptors | Alpha Blockade |
| Causes postural HTN since these vein receptors are blocked. The filling P is low & BP drops. | Postural HTN caused by ALPHA BLOCK |
| Causes epinephrine reversal since blocking this exposes the effect of beta stimulation. Causes dilation of blood vessels in skeletal m & HR will increase | Alpha Blockers |
| Causes radial pupillary muscle to relax causing Miosis (pupil constriction) | Alpha Blocker |
| Vasodilation in nasal mucosa causing nasal stuffiness caused by this | Alpha Blocker |
| Prostate, sphincters & base of bladder relax are widely used for tx of BPH to decrease resistance to urine flow | Alpha Blocker |
| Competitive alpha 1/2 antagonist that DEC peripheral resistance & BP (especially diastolic). Will likely cause Tachycardia | Phentolamine (used rarely) _Side Effects: Tachycardia, arrhtyhmia, MI, HYPOtension, gastric stimulation, abd pain, peptic ulcer |
| Alpha2 block INC NE release stimulating baroreceptor reflex & beta stimulation will prevail, INC HR | Phentolamine (used rarely) _Side Effects: Tachycardia, arrhtyhmia, MI, HYPOtension, gastric stimulation, abd pain, peptic ulce |
| Used rarely. For hypertensive crisis to pheochromocytoma or MAOI. Prevents necrosis after local infusion of alpha agonists | Phentolamine (used rarely) _Side Effects: Tachycardia, arrhtyhmia, MI, HYPOtension, gastric stimulation, abd pain, peptic ulcer |
| Irreversible alpha blockade (very long acting) & tachycardia likely. Most pronounced when standing. Used for pheochromocytoma. | Phenoxybenzime _Side Effects: postural HYPOtension, tachycardia, nasal congestion, inhibit ejaculation, HYPOtension, tachycardia w/epinephrine |
| Sudden onset SEVERE HTN, tachycardia, arrhythmia caused by adrenal tumor releasing NE/Epi. Use Phenoxybenzamine for initial tx, then surgery | Pheochromocytoma _Measure 24hr urine NE & VMA |
| Alpha1 selective that relaxes arterial & venous smooth m, decreasing peripheral resistance. DEC venous return & preload on heart. Lowers tachycardia & may inhibit baroreceptor reflex. Beneficial for lipids | Prazosin (Minipress) _Give twice daily. _DEC BP & HR |
| Similar to prazosin use once a day for BPH or HTN to decrease HR/BP & benign prostatic hyperplasia | Terazosin, Doxazosin _1st Dose Phenomenon:sudden and severe fall in blood pressure that can occur when changing from a lying to a standing position the first time that an alpha blocker drug is used |
| sudden and severe fall in blood pressure that can occur when changing from a lying to a standing position the first time that an alpha blocker drug is used | First dose phenomenon _Seen in Terazosin, Doxazosin |
| Postural HYPOtension & syncope 30-90mins after 1st dose can occur therefore have patient take 1st dose @bedtime, so lying down for some hours. May also happen when dose INC or 2nd drug added | First dose phenomenon _Seen in Terazosin, Doxazosin |
| Side effect of Terazosin, Doxazosin | First Dose Phenomenon Orthostatic HYPOtension (more severe w/Viagra/Nitrates) Dizziness Nasal stuffiness |
| Alpha1 selective impt in prostate. Very good for men who have had postural hypotension w/other alpha blockers. Main side effect is dizziness w/ejaculation | Tamsulosin |
| Alpha1b impt in blood vessels. Very good for men who've have postural hypotension w/other alpha blockers | Tamsulosin _Side effect: dizziness w/ejaculation |
| Blocks alpha2 receptors to INC NE release, BP & HR. Also INC motor activity, tremors | Yohimbine _Sold as "natural" alternative to Viagra but not determined _May interefere w/Clonidine effect! |
| Lowers blood pressure when used chronically, decreases HR & contraction, cardio effects greatest when sympathetic tone is high, rise in HR in response to excercise shortened | Beta Receptor Blockade |
| DEC HR (AV conduction slow, rate of depolarization of ectopic pacemakers reduced). Myocardial contraction DEC, O2 DEC, CO DEC, Renin release DEC | Beta Receptor Blockade |
| Short term: CO decrease, relax skeletal m vasculature by beta2receptors blocked, DEC CO increases SNS input, peripheral resistance INC | Short term beta block effect on BP |
| Long term use of this will DEC BP as peripheral resistance returns to pre-drug value | Long term effect of beta blockers |
| In asthma/COPD patient. Use of these can be fatal (though beta1 selective may be tolerated) | Beta blockers causing bronchoconstriction |
| Decreases formation of aqueous humor. Used topically in glaucoma | Beta blocker in eye _Lowers intraocular pressure |
| Masks sx of hypoglycemia in insulin-dependent DM making it harder to recover from hypoglycemia. | Glycogenolysis inhibition by BETA blockers _Beta1 selective antagonists have less effect on glucose |
| Inhibits lipolysis in fat cells, INC VLDL & DEC HDL. Blocks muscular uptake of K+ | Beta receptor blockade |
| "Membrane stabilizing" via Na channel blockade therefore used in local anesthetics | Beta Blockers |
| Can be used as antiarrhytmic agents | Beta Blockers |
| Should NOT use these topically in the eye since they can cause corneal damage locally | Beta Blockers |
| Competetive beta1/2 antagonist that DEC HR, contractility, renin, lipolysis, glycogenolysis. Used as local anesthetic | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| DEC BP w/CHRONIC use (was once used to tx HTN). Decreases mortality following MI. Improves angina. Antiarrhythmic used in obstructive cardiomyopathy. Use to tx CHF improving long-term survival | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| Decreases mortality after MI | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| DEC HR in HYPERthyroidism. | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| Prevents migraines | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| DEC portal vein pressure, reducing bleeding in cirrhosis | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| Used to DEC SNS sx of stage fright (tremor) | Propranolol _Oral _Low bioavil _Lipid sol (enters CNS): Sedation _Metab in Liver _Can find in extended release prep |
| Biggest side effect of Propranolol | BRONCHOCONSTRICTION!!! -NEVER use in asthma/COPD |
| Side effects of Propranolol | BRONCHOCONSTRICTION Worsen CHF Bradycardia Abrupt discontinuation can cause arrhythmia Sedation, fatigue, depression Be careful w/insulin-dependent DM!!! |
| Because of the decreased glycogenolysis caused by Propranolol, who should you watch out for? | Insulin-Dependent DM |
| Metabolized in the liver, inhibition of CytP450 may INC antiHTN effect/slow heart when interact w/Cimetidine, Chlorpromazine | Propranolol drug interaction |
| INC metabolism via barbituates, phenytoin, rifampin, smoking can effect this drug | Propranolol drug interaction |
| Calcium channel blockers + Propranolol drug interaction | Additive effect! |
| Non-Selective Beta Blocker used in eye to tx Glaucoma or systemically | Timolol _Caution in asthma(may be absorbed) |
| Non-Selective Beta Blocker used long-acting w/little CNS effect | Nadolol |
| Non-Selective Beta Blocker used for antiarrhtyhmic | Sotalol |
| Selective Beta-1 Blockers | Atenolol Bisoprolol Metoprolol |
| Effects heart by DEC HR, contraction force, renin release, BP. Used for HTN tx & INC life-expectancy post-MI | Selective Beta-1 Blockers: Atenolol Bisoprolol Metoprolol |
| Used for migraine prophylaxis | Selective Beta-1 Blockers: Atenolol Bisoprolol Metoprolol |
| No block of beta2 effect on blood vessels to skeletal m. BETTER exercise tolerance & less effect on glycogenolysis therefore safer for DM. Use caution asthma/COPD. Selectivity DEC as dose INC | Selective Beta-1 Blockers: Atenolol Bisoprolol Metoprolol |
| May be safer than Timolol in eye and causes less bronchoconstriction | Betaxolol |
| HIGHLY selective Beta1. Causes NO release-->vasoDILATION. Better effect on BP w/fewer side effects, on lipids & glucose | Nebivolol(Bystolic) |
| VERY short acting beta1 blocker given IV for short effect. Infusion may be continued as long as needed. Used if you want to be able to QUICKLY END the effect | Esmolol (Brevibloc) |
| Partial agonist activity in beta blockers _Pindolol, Carteolol, Penbutolol (non selective) _Acebutolol (selective beta1) | Intrinsic Sympathetic Activity _Stimulates when SNS is low, and blocks when it's high. |
| Stimulates partial agonist behavior when SNS is low, and blocks when it's high. May DEC risk of bronchoCONSTRICT or Bradycardia. May also have less effects on plasma lipids. Used for HTN/Angina. | Intrinsic Sympathetic Activity in beta blockers: _Pindolol, Carteolol, Penbutolol (non selective) _Acebutolol (selective beta1) |
| Non-selective beta block with intrinsic SNS activity (ISA). Used for HTN/Angina. | Pindolol, Carteolol, Penbutolol |
| Used in eye to tx glaucoma, fewer systemic effects than Timolol.Non-selective beta block with intrinsic SNS activity (ISA). | Carteolol |
| Beta-1 selective with intrinsic SNS . Used for HTN/Angina. | Acebutolol |
| Blocks beta1/2/alpha1 receptors. Alpha1 block will decrease peripheral vascular resistance while beta1 block will prevent tachycardia | Labetalol, Carvedilol |
| Used for IV HTN emergency (careful, may cause hepatic issues) | Labetalol _Blocks beta1/2/alpha1 receptors. Alpha1 block will decrease peripheral vascular resistance while beta1 block will prevent tachycardia |
| Used in CHF, post MI | Carvedilol _Blocks beta1/2/alpha1 receptors. Alpha1 block will decrease peripheral vascular resistance while beta1 block will prevent tachycardia |
| DOC for Glaucoma tx | Prostaglanin Analogues (latanoprost-Xalatan) |
| Beta blocker placed INTO eye for glaucoma | Timolol _Side effect: bronchoCONSTRICTION |
| Beta1 selective blocker used in eye for glaucoma w/less side effects than Timolol | Betaxolol |
| These agonists can be used in glaucoma to DEC production of aqueous humor & increase outflow. | Alpha receptor agonists _Apraclonidine (Iopidine) _Brimonidine (Alphagan) |
| These diuretics can be used in glaucoma since DEC production of intraocular fluid | Carbonic Anhydrase Inhibitor Diuretics |
| Used in glaucoma,acts on M receptors to act as cholinergic agonist | Pilocarpine |
| Used in glaucoma,acts on M AND N receptors to act as cholinergic agonist | Carbachol |
| Used in glaucoma,inhibits AChE activity to act as cholinergic agonist | Demecarium Echothiophate Physostigmine |
| Used in glaucoma,inhibits AChE activity to act as cholinergic agonist. VERY long-lasting effect | Echothiophate |
| Not used often because they effect vision (constrict pupil & affect accomodation). Used primarily in NARROW ANGLE Glaucoma | Cholinergic Agonists _Carbachol _Demecarium _Echothiophate(long-lasting) _Physostigmine _Pilocarpine |
| Inhibits NE release from n terminals. Needs to enter presynaptic terminal (cocaine will prevent this effect). Loss of SNS tone will occur over time. | Guanethidine _NO longer used _Severe side effects: postural HTN, DEC in cerebral/coronary blood flow, no ejaculation, diarrhea |
| Why do we no longer use Guanethidine? | Severe side effects: postural HTN, DEC in cerebral/coronary blood flow, no ejaculation, diarrhea |
| DEC uptake & storage of NE in vesicles. Depletes NE, DA & 5HT in both periphery & CNS. Central effects lead to DEC in BP. | Reserpine _Severe diarrhea _Depression, sedation (loss of NE in brain) _Parkinson's effect due to Dopamine depletion |
| Blocks tyrosine hydroxylase which is the rate-limiting step of the formation of I-DOPA from tyrosine. | Metyrosine _Tx of pheochromocytoma if AlphaBlockers cannot control BP |
| Tx of pheochromocytoma if AlphaBlockers cannot control BP | Metyrosine |
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