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Phamacology 400
Drugs and Drug Classes
| Question | Answer |
|---|---|
| How does Herceptin (trastuzumab)work? | - Monoclonal Antibody - Binds with HER2 and prevents it from interacting with other receptors on the cell surface. |
| How does Gleevec (imatinib) work? | - Inhibitor - Inhibits several different proteins, including two proteins involved in growth signaling. |
| How does HGS-ETR1 and -2 work? | - Bind to death receptors 4 and 5. - Trigger the pro-death signaling pathways. |
| How does Avastin (bevacizumab) work? | - Monoclonal Antibody - Binds to VEGF and keeps it away from receptors on the surface of endothelial cells. - New blood vessels are not formed. - Prevent a tumor from growing. |
| How does Nexavar (sorafenib) work? | - Small molecule - Inhibits multiple kinases which blocks the signaling pathways for growth. - Disrupts a tumors recruitment of new blood vessels. |
| Uses of antihistamines | -relief of symptoms associated with seasonal allergic rhinitis -relief of symptoms associated with perennial allergic rhinitis -treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria |
| Mechanism of antihistamines | -antagonists at H1 receptors -prevent histamine from binding to H1 receptors if present before histamine arrives -try to jostle histamine off from H1 receptors if histamine is already there |
| Long term asthma control medications | -Inhaled corticosteroids -Leukotriene modifiers -Long-acting beta-agonists -Cromolyn -Theophylline |
| Quick relief asthma medications | -Short-acting beta-agonists -Systemic corticosteroids |
| Uses of low dose glucocorticoids | -treatment of adrenal cortical insufficiency -replacing missing glucocorticoid |
| Uses of high-dose glucocorticoids | treatment of allergic states usually those not treated by other therapy treatment of auto-immune diseases treatment of inflammatory diseases arthritis recommended only for short-term treatment of dermatologic diseases treatment of leukemias and lym |
| Uses of local glucocorticoids | topical use to treat skin, mucous membrane, and ocular disorders in many creams that can be purchased OTC inhalation use to treat allergic rhinitis and asthma probably most common current use |
| Uses of B2-Adrenergic Agonists | Used to treat asthma / bronchospasm |
| Mechanism of Cysteinyl Leukotrienes | -LTC4, LTD4, and LTE4 -released from mast cells and eosinophil cells -constrict bronchioles -dilate blood vessels -make small blood vessels leaky |
| Mechanism of Muscarinic Receptor Antagonists | antagonize excess parasympathetic nerve activity |
| Uses of Muscarinc Receptor Agonists | -Treat urine retention one-time such as post surgery -Treat open-angle glaucoma -stimulate all muscarinic receptors salivation, tearing, difficulty seeing in dim light, slow heart, constricted bronchials |
| Uses for Acetylcholine Esterase Inhibitors | -useful where activity is present but less than desired -myasthenia gravis (but use better drugs, today) -Alzheimer’s disease |
| Uses of Muscarinic Antagonists | block all muscarinic receptors dry eyes, dry mouth, urine retention, memory loss, disorientation, discomfort in sunlight once in many otc cold and allergy preps treat motion sickness cycloplegia treat over-active bladder( selective M3 antagonists) |
| Uses of Nicotinic Antagonists | Used as paralytic agents for certain kinds of surgery |
| Uses of Non-specific Andrenergic Agonists | Major therapeutic use is to treat shock various agonists (norepinephrine, epinephrine, dobutamine) have differing affinities for types of adrenergic receptors type of shock dictates which agonist is used |
| Mechanism of a1-adrenergic agonists | constrict blood vessels |
| Mechansim of a20adrenergic agonists | in the brain decrease sympathetic tone sedative effect at higher doses |
| Uses of a1-adrenergic agonist | treatment of vascular failure in shock, drug-induced hypotension, or hypersensitivity to overcome paroxysmal supraventricular tachycardia to prolong spinal anesthesia to maintain an adequate level of blood pressure during spinal and inhalation anesthes |
| Uses of B-adrenergic agonist | treat hypovolemic and septic shock treat heart block treat cardiac arrest treat bronchospasm occurring during anesthesia Will affect heart, lung, and metabolic functions |
| Uses of a-adrengeric antagonists | Used to treat benign prostatic hyperplasia |
| Uses of B-adrenergic antagonists | treat hypertension manage angina pectoris control rapid heart beat arrhythmias minimize recurrence of heart attack treatment of congestive heart failure migraine prophylaxis Have anti-anxiety / anti-stress effect |
| Uses of diuretics | treat edema treat hypertension |
| Uses of Angiotension II | Constricts blood vessels blood pressure Stimulates aldosterone secretion from renal cortex aldosterone acts at collecting duct to enhance sodium reabsorption, resulting in urine production net result is blood volume |
| Uses of ACE inhibitors | treatment of hypertension, either alone as initial therapy or concomitantly with other drugs adjunctive therapy in the management of heart failure in patients not responding adequately to diuretics and digitalis |
| Uses of Angiotensin II Receptor agonists | treatment of hypertension alone or in combination with other antihypertensive agents treatment of heart failure (NYHA class II to IV) in patients who are intolerant of angiotensin-converting enzyme (ACE) inhibitors |
| Mechanism of Calcium Channel Antagonists | Interference with calcium channels in smooth muscle decreases amount of muscle contraction results in dilation of blood vessels results in less force of contraction by heart muscles |
| Uses of Calcium Channel Antagonists | treatment of hypertension, alone or in combination with other antihypertensives treatment of chronic stable angina treatment of vasospastic angina |
| Mechansism of nitrate drugs | Release NO (nitric oxide into blood) NO cGMP Ca vasodilation |
| Uses of nitrate drugs | treat angina pectoris |
| Uses of cardiac glycosides | treatment of mild-to-moderate heart failure control of ventricular response rate in patients with chronic atrial fibrillation |
| Mechanism of cardiac glycosides | Positive inotropic effect Slow heart rate |
| Uses of HMG-CoA Reductase inhibitors | Part of chemical structure resembles HMG-CoA Slow HMG-CoA reductase rate of action LDL-cholesterol ~30% HDL-cholesterol ~10% triglygeride ~15% Highly effective at cardiovascular major problems |
| Mechanoism of PPAR-a receptor activator | activation of PPAR-alpha receptor increases activity of lipoprotein lipase changes LDL from small, dense particles to large, buoyant particles ↓ total cholesterol ↓ LDL cholesterol ↓ total triglycerides ↓ VLDL (triglyceride-rich lipoproteins) |
| Mechanism of VLDL secretion inhibitor | decreases VLDL and LDL levels, and Lp(a) in most patients often increases HDL levels significantly niacin |
| Uses of fibronolytic drugs | Steptokinase target is plasminogen converts plasminogen to plasmin plasmin breaks down fibrin Used to dissolve emboli (clots) that are already formed (stroke, heart attack) Mechanical means are often used |
| Mechanism of antiplatelet drugs | antagonist at ADP receptor on platelets ADP normally stimulates platelet aggregations |
| Mechanism of acetylcholine esterase inhibitors | blocks the breakdown of acetylcholine increases amount of acetylcholine at receptors at low doses, thought to maintain normal signal pattern |
| Mechanism of acetylcholine receptor partial agonists | interacts with receptor but produces much lower maximum response than does acetylcholine lessens effect of full agonists through competition for binding sites |
| Mechanisms of GABAergic receptors | receptor operated ion channel gates chloride causes hyperpolarization GABA is major inhibitor neurotransmitter in brain drugs target a modulatory site on receptor complex increase chloride conductance enhance inhibitor effect of GABA |
| Use of sedative-hypnotic and anxiolytic drugs | overall effect of these drugs is to decrease overall brain activity |
| Diseases / conditions / effects controlled or produced by generally slowing down brain activity | anxiety insomnia panic attacks obsessive/compulsive disorder epilepsy unconsciousness for surgery |
| Uses for positive modulators of GABA-A receptors | uses (all benzodiazepines) treat anxiety uses (some benzodiazepines) hypnosis (sleep aid) treat panic attacks pre-operative sedation anesthetic treat epilepsy muscle relaxant |
| Uses of GAGA synapse modifiers | uses: treat partial seizures treat post herpes neuralgia (pain in nerve tracts) unlabeled uses: tremors associated with multiple sclerosis treat neuropathic pain treat bipolar disorder migraine prophylaxis |
| Mechanism of metabotropic receptors | regulate biochemical pathways slower, more sustained responses than receptor operated ion channels modulate how dendrites respond to ion fluxes modulate plasticity |
| Uses of inhibitors or monoamine transporters | serotonin and/or norepinephrine uptake used as anti-depressant drugs used for variety of other mental conditions |
| Uses of inhibitors of dopamine uptake | used to treat attention deficit and hyperactivity disorder (ADHD) and narcolepsy |
| Uses of agonists at dopamine synapses | treat Parkinsons disease dopamine neurons die strategy is to replace lost dopamine – help remaining neurons work better levodopa = made into dopamine strategy is to activate dopamine receptors |
| Uses of agonists at mu-opioid receptors | used to treat pain used to suppress cough used to control diarrhea loperamide (Immodium) does not cross blood-brain barrier |
| Uses of partial agonists at mu-opioid receptors | treat minor pain treat opioid addiction |
| Uses of prostaglandins | relative to pain prostaglandins sensitize pain receptors (detect pain at lower threshold) relative to fever prostaglandins regulate where “thermostat” is set relative to inflammation (swelling) prostaglandins promote inflammation |
| Mechanism of Aspirin-like analgesics | inhibit cyclooxygenase (COX) enzyme often called “non-steroidal anti-inflammatory drugs” NSAIDS analgesic, anti-inflammatory, antipyretic (anti-fever) high doses for prolonged time damage stomach |
| Mechanism of Tylenol-like analgesics | inhibit cyclooxygenase (COX) enzyme analgesic, antipyretic (anti-fever) thought to be metabolized by peroxidase enzyme in inflammed tissue = no anti-inflammatory effect high doses damage liver |
| Uses of proton pump inhibitors | treat ulcers (both gastric and duodenal) short-term treatment of heartburn and other symptoms associated with GERD (gastroesophageal reflux disease) treat erosive esophagitis treat “hyper-secretory” states |
| Mechanism of histamine h2 receptor antagonists | Competitive antagonists of H2 receptor Inhibit >90% of nocturnal acid secretion Primarily histamine mediated Inhibit 60-80% of daytime acid secretion Substantial mediation by gastrin and acetylcholine |
| Uses of H2 antagonists | treat ulcers (both gastric and duodenal) short-term treatment of heartburn and other symptoms associated with GERD (gastroesophageal reflux disease) treat erosive esophagitis treat “hyper-secretory” states |
| Uses of stool softeners | 1-3 days for effect soft stool |
| Uses of anti-arrheals: absorbants | bind water - provide a carrier for excess water |
| Uses of laxatives | Soft or semi-fluid stool in 6-8 hours (mild secretory action) |
| Uses of cathartics | Watery evacuation / 1-3 hours for effect |
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