Block 2 (Anticholinergic drugs) Flashcards
Describe the following for Atropine:
What is it?
- drug type
How does it work?
- MOA
What are the clinical uses?
What are the adverse effects?
Drug type:
Muscarinic antagonist (it is competitive at all M receptors)
MOA:
It antagonizes all the M receptors to produce sympathetic/anti-parasympathetic effects
- Mydriasis/cycloplegia
- Bronchodilation
- Less peristalsis
- Urine retention
- Higher HR & AV/SA nodal conduction
Clinical uses:
1) Bradycardia
2) Opthalmic applications (long action)
3) Antispasmodic
4) Antisecretory
5) AChE inhibitor OD
6) Antidiarrheal
Adverse effects:
Higher body temp (hyperthermia in infants)
Tachycardia
Dry mouth
Flushed/dry skin
Cycloplegia (paralyzed accommodation)
Constipation
Urinary retention (in BPH)
Acute angle glaucoma (in elderly)
Disorientation
Drug type:
Muscarinic antagonist (it is competitive at all M receptors)
MOA:
It antagonizes all the M receptors to produce sympathetic/anti-parasympathetic effects
- Mydriasis/cycloplegia
- Bronchodilation
- Less peristalsis
- Urine retention
- Higher HR & AV/SA nodal conduction
Clinical uses:
1) Bradycardia
2) Opthalmic applications (long action)
3) Antispasmodic
4) Antisecretory
5) AChE inhibitor OD
6) Antidiarrheal
Adverse effects:
Higher body temp (hyperthermia in infants)
Tachycardia
Dry mouth
Flushed/dry skin
Cycloplegia (paralyzed accommodation)
Constipation
Urinary retention (in BPH)
Acute angle glaucoma (in elderly)
Disorientation
Describes which medication?
Atropine
What are the clinical uses of atropine?
Clinical uses:
1) Bradycardia
2) Opthalmic applications (long action)
3) Antispasmodic
4) Antisecretory
5) AChE inhibitor OD
6) Antidiarrheal
What are the adverse side effects of atropine?
Adverse effects:
Higher body temp (hyperthermia in infants)
Tachycardia
Dry mouth
Flushed/dry skin
Cycloplegia (paralyzed accommodation)
Constipation
Urinary retention (in BPH)
Acute angle glaucoma (in elderly)
Disorientation
What are the physiological effects of atropine?
Hot as a hare: increased body temperature
Blind as a bat: mydriasis (dilated pupils)
Dry as a bone: dry mouth/eyes/decreased sweat
Red as a beet: flushed face
Mad as a hatter: delirium
Atropine
Cyclopentolate
Homatropine
Scopolamine
Tropicamide
All cause ______ & _______
They can all be used to treat which condition?
Cause:
Mydriasis
Cycloplegia
Rx:
Uveitis
These drugs cause cycloplegia & mydriasis & can be used to treat uveitis
Atropine
Cyclopentolate
Homatropine
Scopolamine
Tropicamide
Solenfenacin
Oxybutynin
Flavoxate & Festerodine
Tolterodin & Trospium chloride
Darifenacin
Are all what type of drug used to treat which condition?
Vesicoselective drugs that can be used to treat overactive bladder syndrome
How do muscarinic antagonists treat Overactive Bladder syndrome/urgency incontinence?
The muscarinic antagonists like Oxybutynin inhibit M3 receptors in the bladder causing smooth muscle relaxation to reduce urination urgency
How do muscarinic agonists treat urinary retention?
Muscarinic agonists like bethanechol act as Ach at M receptors to activate them causing smooth muscle contraction & urination
How do sympathomimetics treat Overactive Bladder syndrome/urgency incontinence?
Sympathomimetics like mirabegron B3 agonists which relax detrusor muscle to increase retention (no peeing)
How do a1-blockers treat BPH?
alpha 1 blockers like tamsulosin inhibit alpha 1 receptors to relax the smooth muscle in the bladder neck & prostate to lessen the urinary obstruction
Describe the following for Oxybutynin:
What is its MOA?
What is its clinical uses?
How is it administered?
MOA:
It has a high affinity for M1/M3 receptors in the salivary glands & bladder
Clinical uses:
1) Urinary frequency/urge incontinence (overactive bladder)
2) Nocturnal enuresis (bedwetting)
Administered orally
Describe the following for Tolterodine:
What is its MOA?
What is its clinical uses?
MOA:
It targets the M3 receptors in the detrusor muscles to relax it (minimal anticholinergic side effects) & it’s then metabolized by CYP3A4
Clinical use:
1) Urinary frequency/urge incontinence (overactive bladder)
When is atropine use contraindicated?
Glaucoma
BPH
Pyloric obstruction (pylorospasm)
Describe the following for scopolamine:
What is the MOA?
What are the clinical uses?
What are the side effects?
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical uses:
1) Motion sickness
Side effects:
1) Sedation
2) Short-term memory block
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical uses:
1) Motion sickness
Side effects:
1) Sedation
2) Short-term memory block
Describes which drug?
Scopolamine
Describe the following for atropine:
What is the MOA?
What are the clinical uses?
What are the side effects?
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical uses:
1) Antispasmodic
2) Antisecretory
3) Managing AChE inhibitor overdose
4) Antidiarrheal
5) Ophthalmology (test accommodation but it lasts a few days so it’s not preferred)
Side effects:
High body temp
Dry skin(flushed)/eyes/mouth
Mydriasis
Delirium
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical uses:
1) Antispasmodic
2) Antisecretory
3) Managing AChE inhibitor overdose
4) Antidiarrheal
5) Ophthalmology (test accommodation but it lasts a few days so it’s not preferred)
Side effects:
High body temp
Dry skin(flushed)/eyes/mouth
Mydriasis
Delirium
Describes which drug?
Atropine
Describe the following for Tropicamide:
What is the MOA?
What is a clinical use?
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical use:
Ophthalmology (topical)
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical use:
Ophthalmology (topical)
Describes which drug?
Tropicamide
Describe the following for Ipratropium & Tiotropium:
What is the MOA?
What are the clinical uses?
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical use:
Asthma & COPD (doesn’t enter the CNS)
MOA:
An M antagonist that results in sympathetic-like effects (blocks Ach)
Clinical use:
Asthma & COPD (doesn’t enter the CNS)
Describes which drugs?
Ipratropium & Tiotropium
Describe the following for Benztropine & Trihexyphenidyl:
What is the MOA?
What are the clinical uses?
MOA:
A lipid soluble M antagonist that can enter the CNS & cause sympathetic-like effects (blocks Ach)
Clinical use:
1) Parkinsonism
2) Acute extrapyramidal symptoms
MOA:
A lipid soluble M antagonist that can enter the CNS & cause sympathetic-like effects (blocks Ach)
Clinical use:
1) Parkinsonism
2) Acute extrapyramidal symptoms
Describes which drugs?
Benztropine & Trihexyphenidyl
Describe the following for Oxybutynin:
What is the MOA?
What is the clinical use?
MOA:
An M antagonist that causes sympathetic-like effects (blocks Ach)
Clinical use:
1) Overactive bladder syndrome (urge incontinence)
Describe the following for Hexamethonium & mecamylamine:
What are they?
What do they do?
They are nicotinic receptor antagonists that block the ganglion & reduce autonomic tone thereby preventing baroreceptor reflex changes in heart rate
They are nicotinic receptor antagonists that block the ganglion & reduce autonomic tone thereby preventing baroreceptor reflex changes in heart rate
Describes which drugs?
Hexamethonium & mecamylamine
What are the effects of ganglion blocking agents (like Hexamethonium & mecamylamine)?
Arterioles
Veins
Heart
Iris
Ciliary muscle
Gi
Bladder
Salivary
Sweat
Arterioles = Vasodilation & hypotension
Veins = Dilation to decrease venous return & co
Heart= Tachycardia
Iris= Mydriasis
Ciliary muscle= Cycloplegia
Gi= Constipation
Bladder= Urinary retention
Salivary= Xerostomia
Sweat= Anhidrosis
High Urination in the human subject is decreased by
A. Muscarinic agonists
B. Muscarinic antagonists
C. AChase inhibitors
D. Nicotinic agonists
E. Nicotinic antagonist
B. Muscarinic antagonists
A child presented with history of ingestion of some unknown plant and developed mydriasis, tachycardia, dry mouth, warm skin and delirium. Which of the following group of drugs is likely to be responsible for
the symptoms of this child?
(a) Atropine poisoning
(b) Carbamates Poisoning
(c) Organophosphate poisoning
(d) Benzodiazepine
(a) Atropine poisoning
Prior to an eye exam a patient is given a drug that causes mydriasis but has no effect on accommodation (Without cycloplegia). What is the most likely identity of this drug?
A. mecamylamine
B. neostigmine
C. pilocarpine
D. phenylephrine
E. tropicamide
D. phenylephrine
You are being asked to give your expert opinion as a toxicologist regarding an effective antidote for belladonna (Atropine) poisoning. Which of the following agents would you suggest?
(a) Neostigmine
(b) Physostigmine
(c) Pilocarpine
(d) Methacholine
(b) Physostigmine
Researcher who is interested in creating an anticholinergic agent that would be useful in patients with irritative bladder symptoms would be interested in targeting which of the following receptors?
(A) M1
(B) M2
(C) M3
(D) M4
(E) M5
(C) M3
A 55-year-old woman comes to the physician’s office complaining of episodic loss of urine for the last one month. She states that these episodes occur almost every day and are very embarrassing. They begin as an urge to urinate, and most of the time she cannot make it to the bathroom before urinating on herself. Physical examination, including pelvic examination, is unremarkable. A urinalysis is within normal limits. Urodynamic evaluation is significant for detrusor instability. Initial non-pharmacologic measures are unsuccessful and pharmacologic therapy is considered. The appropriate treatment for this patient’s condition includes an agent that affects which of the following?
A.Antagonism of alpha-1 adrenoreceptors
B.Antagonism of beta-1 adrenoreceptors
C.Antagonism of muscarinic cholinergic receptors
D.Antagonism of nicotinic cholinergic receptors
E.Stimulation of alpha-2 adrenoreceptors
F.Stimulation of beta-2 adrenoreceptors
C. Antagonism of muscarinic cholinergic receptors
