Anti-cholinergic drugs Flashcards
atropine is classified as a _____ drug and a ___ ___
anti-muscarinic; tertiary amine
scopolamine is classified as a ____ drug and a ____ ___
anti-muscarinic; tertiary amine
homatropine is classified as a ____ drug and a ____ ____
anti-muscarinic; tertiary amine
Dariferain is classified as a _____ drug and a ____ ____
anti-muscarinic; tertiary amine
Benztropine is classified as a ____ drug and a ____ ____
Anti-muscarinic, tertiary amine
Glycopyrrolate is classified as a _____ drug and a ____ ____ ___
anti-muscarinic; quaternary ammonium compound
Ipratropium is classified as a ______ drug and a ____ ___ ___
anti-muscarinic; quaternary ammonium compound
Nicotine is classified as a ____ _____
Ganglionic stimulant
Mecamylamine is classified as a ____ ___
ganglionic blocker
Nicotine at lower doses has a _____ effect
agonist effect
Nicotine at higher doses has a ____ ____
depolarizing blockade
Atropine and scopolamine are ____ ______ found in several plants
Atropine and scopolamine are natural alkaloids found in several plants
M1, M2, and M3 receptors have a ____ affinity for atropine
high
M3 has ____ affinity and M1 and M2 have ____ affinity for Darifenacin
high;little to no
M1, M2, and M3, have a ____ affinity for Glycopyrrolate, Ipratropium
high
Nicotinic receptors have a ____ affinity for Glycopyrrolate, Ipratropium
moderate
Tolterodine, M3-selective antimuscarinic, to treat overactive _____
Tolterodine, M3-selective antimuscarinic, to treat overactive bladder
- 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.
- 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.
Atropine and scopolamine block ______subgroups of M receptors
•Atropine and scopolamine block all subgroups of M receptors
Tertiary antimuscarinic drugs have ______blocking activity at ganglionic Nn receptors.
Tertiary antimuscarinic drugs have negligible blocking activity at ganglionic Nn receptors.
Quaternary compounds mainly block ______ receptors but also exhibit a significant blocking activity at _____ ____receptors
Quaternary compounds mainly block muscarinic receptors but also exhibit a significant blocking activity at ganglionic Nn receptors
Oral bioavailability: variable (atropine _____; ipratropium >____)
Oral bioavailability: variable (atropine 50%; ipratropium >1%)
Distribution
- Tertiary amines distribute in _____tissues.
- Quaternary derivatives do not enter the _____.
Distribution
- Tertiary amines distribute in all tissues.
- Quaternary derivatives do not enter the CNS.
Biontransformation
•~ 50% of atropine and 90% of scopolamine are metabolized by the _________
Biontransformation
•~ 50% of atropine and 90% of scopolamine are metabolized by the liver.
Excretion
- About 60% of atropine is excreted by the ______.
- Half-lives: Atropine and scopolamine: ~____ hours; Glycopyrrolate: ~ ___ hours
Excretion
- About 60% of atropine is excreted by the kidney.
- Half-lives: Atropine and scopolamine: ~3 hours; Glycopyrrolate: ~ 10 hours
•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.
•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.
•Atropine has a good therapeutic index in adults, but a dose of ____ mg can be lethal for children.
•Atropine has a good therapeutic index in adults, but a dose of 5 mg can be lethal for children.
- 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.
- 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.
- 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.
- Diagnosis of poisoning by anti-muscarinic drugs is easy in severe cases. An IM injection of physostigmine 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.
symptomatic treatment of anti-muscarinic drug poisoning
- Maintenance of vital signs
- Alleviation of convulsion with _____
- _____ control with ice bags and alcohol sponges.
symptomatic treatment of anti-muscarinic poisoning:
- Maintenance of vital signs
- Alleviation of convulsion with diazepam
- Temperature control with ice bags and alcohol sponges.
Poisoning with anticholinergics:
____: 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
Poisoning with anti-cholinergics:
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
Contraindications of anti-muscarinics:
–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
contraindications of anti-muscarinics:
–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
–Hyperthyroidism
–Children
–Elderly
Scopalamine is used for _____ sickness prevention and treatment
motion
What drug do you use for these conditions?:
Visceral hypermolity and spasms
Excessive salivation
Cardiovascular disorders
Cholinesterase inhibitor overdose
Opthalmology
Preanesthetic medication
atropine
What drug do you use for these conditions?
Motion sickness
Opthalmology
Preanesthetic medication
scopalamine
What drug do you use for these conditions?
Opthalmology
homatropine
What drug do you use for these conditions?
Neurogenic bladder
Urinary urge incontinence
Darifenacin
what drug do you use for parkinson’s disease?
Benztropine
What drug do you use for these conditions?
Visceral hypermotility and spasms
Cardiovascular disorders
Preanesthetic medication
glycopyrrolate
What drug do you use for bronchospastic disorders?
Ipratropium
ganglionic blocking drugs mechanism:
–_____blockade of nicotinic receptors (Nn) in:
a) ______ ganglia
b) adrenal medulla
c) ______ nerve terminals
d) central nervous system (mecamylamine)
ganglionic blocking drugs mechanism:
–Competitive blockade of nicotinic receptors (Nn) in:
a) autonomic ganglia
b) adrenal medulla
c) presynaptic nerve terminals
d) central nervous system (mecamylamine)
Ganglionic blocking drugs cardio effects:
- 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 ____.
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.
- Hexamethonium is a ____ _____ (negligible oral absorption and access to the CNS).
- Mecamylamine is a ___ ____ (it is active by oral route and enters the brain).
- 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).
