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WAKA PHARM
PHARM FINAL
Question | Answer |
---|---|
Atropine | Tertiary agent; treat bradycardia and pre-op agent to decrease secretions; myodriatic. |
Atropine | Important in AcHE toxicity to counteract excessive AcH. |
Scopolomine | crosses blood brain barrier; uses: motion sickness by blocking output to vomiting center; PARKINSONISM; decreases bronchial secretions. |
Benztopine mesylate (Cogentin) | synthetic; uses PARKINSONS syndrome+ antpsychotic induced extrapyramidal symptoms. |
Benztopine mesylate (Cogentin) | decreases cholinergic activity in parkinsons; blocks dopamine reuptake prolonging dopamine. |
Trihexyphendryl | uses PARKINSONS and dopamine reuptake; direct antispasmadic on smooth muslces |
Trihexphendryl | small doses produce minor CNS depressant and longer doses can cause atropine like effects. Tolerance is seen with prolonged use. |
Dicyclomine (Bentyl) | Effects on the GI tract due to antimuscarinic effects and direct action on smooth muscles of GI tract. |
Dicyclomine (Bentyl) | uses are antispasmodic in treatment of irritable bowel syndrome. |
Darifencin (Enablex) | uses for over active bladder and urgency. Patient can have increased occurrence of urinary tract infections. |
Homatropine (Isopto Homatopine) | similar structure to atropine; uses produce mydriasis and cycloplegia. CONTRAINDICATED in glaucoma or sensitivity to anticholinergics. Increases IOP. |
Cyclopentolate (cyclogyl) | imilar structure to atropine; uses produce mydriasis and cycloplegia. CONTRAINDICATED in glaucoma or sensitivity to anticholinergics. Increases IOP. |
Tropicamide (mydriacyl) | imilar structure to atropine; uses produce mydriasis and cycloplegia. CONTRAINDICATED in glaucoma or sensitivity to anticholinergics. Increases IOP. |
Glycopyrolate (Robinul) | blocks the effects of vagal stimulation during surgery; blocks the muscarinic stimulation with anticholinesterase. |
Glycopyrolate (Robinul) | uses treat bronchospasms and GI antispasmodic. preop medication that decrease saliva, GI and pulmonary secretions, and decrease acid production. |
Ipratoprium | quaternary agent; structurallly similar to atropine; route is oral or inhalational. Uses: nasal spray for rhinnorhea, bronchodilator for COPD; superior than albuterol, but not as good as other Beta 2 adrenergic agents. |
Propantheline Bromide | older drug not used as much. absorption is incomplete. Uses: duodenal ulcers and irritable bowel syndrome. |
What 3 cholinergic antagonist drugs treat Parkinsons syndrome? | Scopolamine, Benztropine, and Trihexphendryl |
What 3 tertiary cholinergic antagonists agents produce mydriasis and cycloplegia and are contraindicated in patients with glaucoma or those sensitive to anticholinergics? | Hematropine, Cyclopentolate, Tropicamide |
What are the 3 quaternary cholinergic antagonists? | Glycopyrolate, Ipratropium, and Propantheline Bromide |
What do cholinergic antagonists do? | block the action of AcH at muscarinic receptors |
Ganglionic blocker actions are complex and unpredictable. T or F | True |
Trimethaphan | ganglionic blocker that competitively blocks Ach from getting to receptors in the ganglia. |
Hexamethonium | blocks the ion channel after it opens--like a plug. Symptoms are due to blockade of the predominate tone on each tissue. Allows the non-predominant autonomic effects to be expressed. |
Cholinergic Agonists= parasympathomimetic= acetylcholinesterase inhibitors. T or F | True |
Acetylcholine (Michol-E) | uses: opthalmic for glaucoma or eye surgery (cataracts); produces miosis. |
Methacholine (provocholine) | uses: diagnosis of airway hyperreactivity in asthmatics who do not show symptoms. Inhalational route |
Carbachol (miostat) | resistant to acute hydrolysis r/t carbamyl group. uses: antiglaucomic effects |
Bethanchol (Urecholine) | contains a B-methyl group and carbamyl group. Very slowly hydrolyzed by AcHe. uses: paraplegics for urine retention and stimulates GI motility . Counteracts side effects of tricyclic antidepressants. can be used for postpartum |
Pilocarpine (salagen tabs) | alkaloid/synthetic used for open and closed angle glaucoma. used as a miotic for exam/surgery. Salagen tabs used for Sjorgens syndrome. |
Sjorgens Syndrome | chronic automimmune disorder effecting the exocrine glands. |
Muscarine | muscarinic agonist only |
Arecholine | betal nut. no therapeutic used. CNS effects similar to nicotine. |
What are the 2 Irreversible AcHe Inhibitors | Echothiophate (phospholine) and Malathion (ovide) |
Echothiophate | Organophosphate: uses: miotic agent for glaucoma diagnosis. CARE must be taken for cardiac and asthmatic patients. Produces bronchoconstriction. Long term use can produce cataracts. |
Malathion (ovide) | Organophosphate: used as a bug spray. uses: lice and parasites. topical agent and the least toxic to humans. Poisoning is treated with atropine or pralidoxime. |
N1 receptor found where? | found at the autonomic ganglia and neurons. |
N1 receptor blocker by? | hexamethonium (non depolarizing) |
N2 receptor found where? | neuromuscular junction |
N2 receptor blocked by? | d-tubocurarine (non-depolarizing) |
Nicotinic receptors are located where? | sympathetic and parasympathetic ganglion and neuromuscular junctions. |
Neuromuscular nicotinic receptors stimulated by? | nicotine and ACh. |
What is the selective agonist for nicotinic receptors? | phenyltrimethyl ammonium |
What is the non depolarizing antagonist for nicotinic receptors | D-tubocurarine |
What is an almost irreversible antagonist on nicotinic receptors? | alpha-bungarotoxin |
Autoreceptors | mainly muscarinic, inhibit release of ACh, nicotinic autoreceptors found, but they tend to increase rather than inhibit ACh release. |
Nicotinic autoreceptors decrease ACh release? T or F | False |
agents that block the action of ACh at muscarinic receptors? | Cholinergic Antagonists |
What are the other drug classes that have anticholinergic effects? | H1-blockers, phenothiazines, TCA's and carbamazepine (tegretol) |
Anticholinergic toxicity symptoms are? | hyperthermia, mydriasis and cycloplegia, CNS stimulation, and xerostomia. |
AChE, is an enzyme, that has an ionic site which helps attract and hold the positively charged quaternary amine group of ACh in place so the ACh ester group is directed to the esteratic site on the enzyme. T or F? | True |
The esteratic site of AChE contains a polythyrine group which provides the sites esteratic functions, which allows splitting of ACh into choline and acetic acid. T or F? | False |
AChE-Inhibitors act as___________in the autonomic system and as ________ stimulants in the somatic system. | parasympathomimetics; neuromuscular |
Edrophonuium produces reversible inhibition of acetylcholinesterase by electrostatic attachment to the anionic site and hydrogen bonding at the esteratic site of the enzyme. T or F | True |
What acetylcholinesterase drugs produce reversible inhibition of acetylcholinesterase by forming carbamyl-ester complex at the esteratic site of the enzyme. | physostigmine, neostigmine, and pyridostigmine. |
Treatment for organophosphate poisoning involves the use of the anticholinergic__________ and the administration of the enzyme reactivator known as___________ | atropine; pralidoxime |
Pralidoxime only works if the attached OP has not yet aged? T or F | True |
If the attached OP has aged the strong nucleophilic attack of Pralidoxime cannot restore the phosphorylated enzyme to normal. T or F | True |