Anti-cholinergic drugs

Question 1

atropine is classified as a _____ drug and a ___ ___

Answer 1

anti-muscarinic; tertiary amine

Question 2

scopolamine is classified as a ____ drug and a ____ ___

Answer 2

anti-muscarinic; tertiary amine

Question 3

homatropine is classified as a ____ drug and a ____ ____

Answer 3

anti-muscarinic; tertiary amine

Question 4

Dariferain is classified as a _____ drug and a ____ ____

Answer 4

anti-muscarinic; tertiary amine

Question 5

Benztropine is classified as a ____ drug and a ____ ____

Answer 5

Anti-muscarinic, tertiary amine

Question 6

Glycopyrrolate is classified as a _____ drug and a ____ ____ ___

Answer 6

anti-muscarinic; quaternary ammonium compound

Question 7

Ipratropium is classified as a ______ drug and a ____ ___ ___

Answer 7

anti-muscarinic; quaternary ammonium compound

Question 8

Nicotine is classified as a ____ _____

Answer 8

Ganglionic stimulant

Question 9

Mecamylamine is classified as a ____ ___

Answer 9

ganglionic blocker

Question 10

Nicotine at lower doses has a _____ effect

Answer 10

agonist effect

Question 11

Nicotine at higher doses has a ____ ____

Answer 11

depolarizing blockade

Question 12

Atropine and scopolamine are ____ ______ found in several plants

Answer 12

Atropine and scopolamine are natural alkaloids found in several plants

Question 13

M1, M2, and M3 receptors have a ____ affinity for atropine

Answer 13

high

Question 14

M3 has ____ affinity and M1 and M2 have ____ affinity for Darifenacin

Answer 14

high;little to no

Question 15

M1, M2, and M3, have a ____ affinity for Glycopyrrolate, Ipratropium

Answer 15

high

Question 16

Nicotinic receptors have a ____ affinity for Glycopyrrolate, Ipratropium

Answer 16

moderate

Question 17

Tolterodine, M3-selective antimuscarinic, to treat overactive _____

Answer 17

Tolterodine, M3-selective antimuscarinic, to treat overactive bladder

Question 18

• All antimuscarinic drugs ______ _____ muscarinic receptors
• The effectiveness of this blockade (the affinity for the receptor) varies with the antagonist and with the _____ of the tissue.

Answer 18

• All antimuscarinic drugs competitively block muscarinic receptors
• The effectiveness of this blockade (the affinity for the receptor) varies with the antagonist and with the sensitivity of the tissue.

Question 19

Atropine and scopolamine block ______subgroups of M receptors

Answer 19

•Atropine and scopolamine block all subgroups of M receptors

Question 20

Tertiary antimuscarinic drugs have ______blocking activity at ganglionic Nn receptors.

Answer 20

Tertiary antimuscarinic drugs have negligible blocking activity at ganglionic Nn receptors.

Question 21

Quaternary compounds mainly block ______ receptors but also exhibit a significant blocking activity at _____ ____receptors

Answer 21

Quaternary compounds mainly block muscarinic receptors but also exhibit a significant blocking activity at ganglionic Nn receptors

Question 22

Oral bioavailability: variable (atropine _____; ipratropium >____)

Answer 22

Oral bioavailability: variable (atropine 50%; ipratropium >1%)

Question 23

Distribution

• Tertiary amines distribute in _____tissues.
• Quaternary derivatives do not enter the _____.

Answer 23

Distribution

• Tertiary amines distribute in all tissues.
• Quaternary derivatives do not enter the CNS.

Question 24

Biontransformation

•~ 50% of atropine and 90% of scopolamine are metabolized by the _________

Answer 24

Biontransformation

•~ 50% of atropine and 90% of scopolamine are metabolized by the liver.

Question 25

Excretion ## Footnote * About 60% of atropine is excreted by the \_\_\_\_\_\_. * Half-lives: Atropine and scopolamine: ~\_\_\_\_ hours; Glycopyrrolate: ~ ___ hours

Answer 25

Excretion ## Footnote * About 60% of atropine is excreted by the **_kidney_**. * Half-lives: Atropine and scopolamine: ~**_3_** hours; Glycopyrrolate: ~ **_10_** hours

Question 26

•When atropine is used to treat diarrhea, the appearance of \_\_\_\_\_\_is considered a side effect, but when the same drug is used to counteract sinus bradycardia, the appearance of _____ is regarded as a side effect.

Answer 26

•When atropine is used to treat diarrhea, the appearance of **_tachycardia_** is considered a side effect, but when the same drug is used to counteract sinus bradycardia, the appearance of **_constipation_** is regarded as a side effect.

Question 27

•Atropine has a good therapeutic index in adults, but a dose of ____ mg can be lethal for children.

Answer 27

•Atropine has a good therapeutic index in adults, but a dose of **_5_** mg can be lethal for children.

Question 28

* In serious atropine poisoning symptoms and signs appears within \_\_\_\_\_\_minutes after ingestion and may last \_\_\_\_\_days. * Death due to _____ failure may follow a period of circulatory collapse/coma.

Answer 28

* In serious atropine poisoning symptoms and signs appears within **_30-60_** minutes after ingestion and may last **_2-7_** days. * Death due to **_respiratory_** failure may follow a period of circulatory collapse/coma.

Question 29

* Diagnosis of poisoning by anti-muscarinic drugs is easy in severe cases. An IM injection of ______ may be used for confirmation. If signs of _____ activation do not occur poisoning with antimuscarinic drug is almost certain. * The treatment is \_\_\_\_\_. Physostigmine is reserved for severe cases since drug can be more dangerous and no more effective than symptomatic treatment.

Answer 29

* Diagnosis of poisoning by anti-muscarinic drugs is easy in severe cases. An IM injection of **_physostigmin_**e may be used for confirmation. If signs of **_muscarinic_** activation do not occur poisoning with antimuscarinic drug is almost certain. * The treatment is **_symptomatic_**. Physostigmine is reserved for severe cases since drug can be more dangerous and no more effective than symptomatic treatment.

Question 30

symptomatic treatment of anti-muscarinic drug poisoning * Maintenance of vital signs * Alleviation of convulsion with \_\_\_\_\_ * \_\_\_\_\_ control with ice bags and alcohol sponges.

Answer 30

symptomatic treatment of anti-muscarinic poisoning: * Maintenance of vital signs * Alleviation of convulsion with **_diazepam_** * **_Temperature_** control with ice bags and alcohol sponges.

Question 31

Poisoning with anticholinergics: ## Footnote \_\_\_\_: due to vasodilation (cause unknown) \_\_\_\_: due to vasodilation & hyperthermia \_\_\_: due to reduced sweating, reduced salivation, reduced fluid intake & developing dehydration \_\_\_\_: due to cycloplegia and mydriasis \_\_\_\_: due to delirium

Answer 31

Poisoning with anti-cholinergics: ## Footnote RED: due to vasodilation (cause unknown) HOT: due to vasodilation & hyperthermia DRY: due to reduced sweating, reduced salivation, reduced fluid intake & developing dehydration BLIND: due to cycloplegia and mydriasis MAD: due to delirium

Question 32

Contraindications of anti-muscarinics: ## Footnote –Glaucoma –Prostatic \_\_\_\_\_\_ –Urinary tract obstruction –Gastrointestinal tract obstruction –Adynamic ileus –Gastric ulcer –Severe infectious \_\_\_\_\_ –\_\_\_\_\_esophagitis –Ulcerative colitis, Crohn’ disease (toxic _____ can ensue) –Tachyarrhythmias –Coronary artery disease, cardiac failure –\_\_\_\_\_thyroidism –Children –Elderly

Answer 32

contraindications of anti-muscarinics: ## Footnote –Glaucoma –Prostatic **_hypertrophy_** –Urinary tract obstruction –Gastrointestinal tract obstruction –Adynamic ileus –Gastric ulcer –Severe infectious **_diarrhea_** –**_Reflux_** esophagitis –Ulcerative colitis, Crohn’ disease (toxic **_megacolon_** can ensue) –Tachyarrhythmias –Coronary artery disease, cardiac failure –**_Hyper_**thyroidism –Children –Elderly

Question 33

Scopalamine is used for _____ sickness prevention and treatment

Answer 33

motion

Question 34

What drug do you use for these conditions?: ## Footnote Visceral hypermolity and spasms Excessive salivation Cardiovascular disorders Cholinesterase inhibitor overdose Opthalmology Preanesthetic medication

Answer 34

atropine

Question 35

What drug do you use for these conditions? ## Footnote Motion sickness Opthalmology Preanesthetic medication

Answer 35

scopalamine

Question 36

What drug do you use for these conditions? ## Footnote Opthalmology

Answer 36

homatropine

Question 37

What drug do you use for these conditions? ## Footnote Neurogenic bladder Urinary urge incontinence

Answer 37

Darifenacin

Question 38

what drug do you use for parkinson's disease?

Answer 38

Benztropine

Question 39

What drug do you use for these conditions? ## Footnote Visceral hypermotility and spasms Cardiovascular disorders Preanesthetic medication

Answer 39

glycopyrrolate

Question 40

What drug do you use for bronchospastic disorders?

Answer 40

Ipratropium

Question 41

ganglionic blocking drugs mechanism: ## Footnote –\_\_\_\_\_blockade of nicotinic receptors (Nn) in: a) ______ ganglia b) adrenal medulla c) ______ nerve terminals d) central nervous system (mecamylamine)

Answer 41

ganglionic blocking drugs mechanism: –Competitive blockade of nicotinic receptors (Nn) in: a) **_autonomi_**c ganglia b) adrenal medulla c) **_presynaptic_** nerve terminals d) central nervous system (mecamylamine)

Question 42

Ganglionic blocking drugs cardio effects: ## Footnote * Moderate _____ in heart rate * \_\_\_\_\_cardiac output (in spite of the increase in heart rate, because the peripheral venous pooling decreases the preload). * Marked _____ in venous tone and peripheral vascular resistance (which leads to hypotension, mainly in the upright position). * Skin blood flow is \_\_\_\_, splanchnic and renal blood flow are \_\_\_\_.

Answer 42

Ganglionic blocking drugs cardio effects: * Moderate **_increase_** in heart rate * **_Decreased_** cardiac output (in spite of the increase in heart rate, because the peripheral venous pooling decreases the preload). * Marked **_decrease_** in venous tone and peripheral vascular resistance (which leads to hypotension, mainly in the upright position). * Skin blood flow is **_increased_**, splanchnic and renal blood flow are **_decreased._**

Question 43

* Hexamethonium is a ____ \_\_\_\_\_ (negligible oral absorption and access to the CNS). * Mecamylamine is a ___ \_\_\_\_ (it is active by oral route and enters the brain).

Answer 43

* Hexamethonium is a **_quaternary ammonium_** (negligible oral absorption and access to the CNS). * Mecamylamine is a **_secondary amine_** (it is active by oral route and enters the brain).