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Pharmacology (MARB) > Anti Muscarinics Flashcards > Flashcards

Anti Muscarinics Flashcards

1
Q

semi synthetic tertiary antimuscurinic drug used for intestinal spasm

A

Dycycloverin ( dycyclomine)

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2
Q

list all the centrally actin antimuscarinic drugs

A

Biperiden, benztropine, diphenhydramine (for more dramatic response), trihexyphenidyl

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3
Q

drugs that selectively block M3 receptors and are used for the treatment of overactive bladder

A

Darifenacin, solifenacin, imidafenacin

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4
Q

true or false. Tiotropium, oxytropium, aclidinium, and ipratropium are used for treating COPD and asthma

A

false. Aclidium is not used as treatment for asthma. Ipratropium, tiotropium, oxytropium- for asthma

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5
Q

fuction of glycopyrolate

A

used for respiratory disorders

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6
Q

Name the centrally acting antimuscarinic drugs

A

Biperiden, benztropine, diphenhydramine (for more dramatic response), trihexyphenidyl

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7
Q

Name a tertiary antimuscarinic drug with the same function as trospium and homatropine methylbromide

A

Oxybutinin which is used for urinary incontenence. Trospium and Homatropine methylbromide are also used for urinatry incontinence

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8
Q

what type of inhibition does and antimuscarinic drug exhibit?

A

COMPETITIVE INHIBITION. Reversible, equilibrium, surmountable - bind to receptor but no intrinsic activity of its own

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9
Q

True or False. Heteroreceptors are found at the presynapticc muscarinic receptors.

A

False. At Presynaptic muscarinic receptors: autoreceptors | At sympathetic nerve fibers: heteroreceptors

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10
Q

Explain the mechanism of action upon blocking presynaptic M2 receptors

A

Blockade of M2 can augment transmitter release. Presynaptic M2 modulates release of Ach - decreases of Ach - decrease Ach effect. With an antimuscarinic drug blocking the M2 receptor, there is an increase of Ach release.

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11
Q

Explain the paradoxical response occuring upon blocking the M3 receptor

A

antimuscarinic blocks M3 receptors, which result to brochodilation. However, M2 receptor blockade (wherein its function as a modulator of Ach is reduced - inc Ach) can counteract the effect of blocking M3. Blocking M3 results to a paradoxical response of increased levels of Ach - bronchoconstiction

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12
Q

name 4 drugs that possess inverse agonism

A

Atropine, ipratropium glycopyrrolate, trihexyphenidyl

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13
Q

Between atropine and scopolamine, which drug can easily penetrate the blood brain barrier?

A

scopolamine has a greter permeation across BBB than atropin

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14
Q

compare Atropine and Scopolamine in terms of their predilection

A

Atropine - heart, GI,bronsial smooth muscle. Scopolamine: iris sphincter, ciliary muscle, exocrine glands

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15
Q

which drug has a prominent central effects at therapeutic dose? (atropine/scopolamine)

A

Scolpolamine

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16
Q

true or false. Scopolamine exhibits both depression and excitation central effects at a therapeutic dose.

A

True. Excitation is occasionally in presence of severe pain

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17
Q

side effect of using scopolamine as an antiemetic

A

dry mouth

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18
Q

Why use first generation H1 receptor blockers as antiemetic?

A

first genereation H1 receptor blockers have antimuscarinic/atropine like effect

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19
Q

Antimuscarnic drugs that are used for parkinsons disease.

A

centrally acting/ tertiary antimuscarinic drugs ( biperiden, benztropine, diphenhydramine, trihexyphenidyl)

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20
Q

why are the ventricle less affected by the effects of the antimuscarinic drugs?

A

ventricles are less affected due to less vagal parasympathetic control

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21
Q

explain how atropine causes a paradoxical bradycardia at very low dosed given by slow IV.

A

There is a blockade of your prejunctional M1 receptors on the vagal postganglionic fibers that limit Ach release in SA node - Removal of autoinhibition - increased Ach release - bradycardia (but once peripheral effects from atropine takes place, tachycardia occurs)

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22
Q

effects of atropine to the circulation when given alone in clinical doses

A

Atropin counteracts peripheral vasodilation and sharp fall in bp induced by choline esters. M3 in vascular endothelium are not innervated by the parasympathetic system. However, M3 responds to muscarinic agonist. By blocking M3 heteroreceptors antimuscarinic can then counteract vasodilation effects - vasoconstriction

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23
Q

effects of atropine to the circulation when given alone in toxic doses

A

atropine flush

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24
Q

effects of large doses of atropine to the gastrointestinal tract

A

completely abolish Ach on GI motility and secretion only; Decrease amplitude and frequency of propulsive movements means more relaxed walls, Basal secretion is blocked more effectively than that stimulated by food, alcohol, or nicotine

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25
Q

selective M1 antimuscarinic drugs that selectively inhibit gastric acid secretion only

A

pirizepine and telenzepine

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26
Q

which is more selective in blocking M1 receptors? (Telenzepine/pirenzepine)

A

Telenzepine

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27
Q

why is diphenoxylate more effective when taken with atropine in treating traveller’s diarrhea?

A

diphynoxylate can cause dryness of mouth. To prevent this, very low dose of atropin is take.

28
Q

True or false. Effects of endogenous muscarinics are more effectively blocked than those exogenously administered muscarinics.

A

False. Exogenously administered muscarinic stimulants are more effectively blocked than those following vagal impulsive activity/ Parasympathetic nerve activity (edogenous ach)

29
Q

Usage of dicyclomine

A

reduces intestinal spasm

30
Q

nonselective drugs for treating overactive bladder/OAB

A

Tolterodine, oxybutynin, trospium, propiverine

31
Q

selective M3 blockers that are effective in treating overactive bladder

A

Solifenacin, Darifenacin, imidafenacin

32
Q

compare effects of muscarinic agonist and antimuscarinic to the ciliary muscles.

A

muscarinic agonist: cyclopasm; antimuscarinis: cycloplegia

33
Q

effects of antimuscarinis to the ocular system

A

mydriasis, cycloplegia, sandy eyes

34
Q

true or false. Antimuscarinics dilates the eye by acting on the radial muscles

A

False. Antimuscarinics do not stimulate redial muscles

35
Q

explain how antimuscarinics cause mydriasis.

A

recall that Blocking the more dominant division (parasympathetic) - see more effect of the sympathetic system (submissive division. Antimuscarinic inhibits the parasymathetic effect of colinergics (pupillary constriction) making it possible for the sympathetic effect (vasodilation) to be observed

36
Q

which of the following drugs can be used for fundoscopy requiring cycloplegic effects? (Tropicamide/cyclopentylate/Scopolamine/atopine)

A

atropine

37
Q

arrange the following antimuscarinics bsased on their duration of effect in decreasing order. scopolamine, atropine, cyclopentylate, tropicamide, homatropine,

A

Tropicamide: 15-60 mins | Cyclopentylate: 3-6 hrs | Homatropine: 12-24 hrs | Scopolamine: 3-7 days | Atropine: 5-6 days blocked more effectively

38
Q

effect of atropine to the respiratory tract

A

brochodilation. However, it decreases mucociliary clearance and can form a mucous plug (can be a site for bacterial proliferation)

39
Q

what is the advantage of using Ipratropium, oxitropium, and tiotropium over atropine?

A

Less inhibitory effect on mucociliary clearance as compared to atropine. sideeffect: dry mouth

40
Q

how does ipratropium counteract the blockade of m3 receptor-mediated brochoconstriction

A

Ipratropium ounteracts blockade of M3 mediated bronchoconstriction due to removal of autoinhibition by blockin M2 receptor. Ipratropium blocks all muscarinic receptors including presynaptic M2 leading to removal autoinhibition - increase Ach - bronchodilation.

41
Q

compare and contrast therapeutic usage of tiotropim and aclidinium.

A

tiotropium: used for both COPD and asthma; aclidinium: only used for COPD and not for asthma

42
Q

effect of atropine to the exocrine gland

A

xerostomia, anhydrosis, atropine fever (due to the suppression of thermoregulatory sweatin

43
Q

effects of scopolamine to the CNS

A

CNS Depressant (drowsiness, amnesia, fatigue, dremless sleep, decrease REM, suphoria) and anti-emetic

44
Q

centrally acting antimuscarinic drugs

A

Benztropine, biperiden, trihexyphenidyl, procyclidine, diphenhydramine

45
Q

toxic effects of antimuscarinics

A

xerostomia, cycloplegia, atropine flush, atropine fever, cns excitation

46
Q

treatment for atropine taken orally

A

gastric lavage with activated charcoal slurry without delay

47
Q

drugs used for atropine poisoning that can also cross BBB

A

physostigmine

48
Q

Antimuscarinic that is given through IV for sedation and seizures

A

benzodiazepines

49
Q

drugs used for treating antimuscarinic poisoining due to quarternary compounds

A

neostigmine and sympathomimetic

50
Q

list 5 contraindication of antimuscarinics

A

narrow angle glaucoma, benign prostativ hyperplasia, bstructive conditions: urinary tract, GIT, Gastric ulcer, intestinal atony

51
Q

when can anti-muscarinic be used for opthalmologic diagnosis?

A

if cycloplegic or prolonged action is required in fundoscopy

52
Q

what drugs can be used for opthalmologic diagnosis that only require myadriasis?

A

sympathomimetic drugs and alpha adrenoreceptor stimulant (phenylephrine)

53
Q

List some opthalmologic diseases wherein antimuscarinics are used for treatment.

A

anterior uveitis, acute irits, iridocyclitis, keratitis, prevent synechia formation

54
Q

List 4 gastrointestinal disorders that can be treated by antimuscarinics

A

acid peptic disease, common traveller’s diarrhea, intestinal spasm, reflux esophagitis

55
Q

drug used for traveller’s diarrhea that does not have diphynolate

A

lomotil

56
Q

antimuscarinic drug that enhances the gastric emptying time and prevents reflux by increasing the lower esophageal pressure

A

metoclopramide

57
Q

antimuscarinics used for reflux esophagitis

A

metoclopramide and betanechol preferred drug

58
Q

antimuscarinic drugs used for acid peptic disease

A

pirizepine and telenzepine

59
Q

List the therapeutic uses of antimuscarinics in the genitourinary tract

A

urolithiasis, enuresis in childre, urniary incontinence, overactive bladder

60
Q

antimuscarinic drug used to decrease urinary spasm in ureter

A

hyoscine

61
Q

used to relieve bladder spasm after urologic surgery and in reducing involuntary voiding in patinets with neurologic disease

A

oxybutinin

62
Q

antimuscarinic nonselective antagonists with greater selectivity for M3 receptors than oxybutinin or trospium

A

darifenacin and solifenacin

63
Q

a tricyclic antidepressant drugs that is used to reduce incontinence in institutionalized elderly patients

A

impramine

64
Q

antimuscarinic drug used for COPD and has a longer bronchodilation action thatn ipratropium

A

tiotropium.

65
Q

antimuscarinic drug given to patients with mycetism

A

atropine

Pharmacology (MARB) (6 decks)

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