Cholinergic Antagonists Flashcards
1
Q
Atropine
A
- Nonselective Competitive Reversible Antagonist M1/M2/M3
M1 - Sedation + Psychosis
M2 - Tachycardia + Mild vasodilation
M3 - DEC GI motility + Urine Ret + Cycloplegia W/ Mydriasis - Clinical: Cholinesterase Poisoning Antidote; Bradycardia, Urine Incontinence; Mydriasis; Antispasmodic
- Contra: Infants (Hyperthermia); Glaucoma; Pregnancy class B; CHD; AMI, CHF, or hypertension
2
Q
Scopolamine
A
- Nonselective competitive muscarinic antagonist
- Crosses BBB -> Nausea
- Clinical: UI ret; Cycloplegia + Mydriasis; DEC GI mot; Euphoria (Abuse)
- Postoperative Nausea
- Patch
3
Q
COPD + Asthma Musc Antagonist
A
Ipratropium
Tiotropium
Glycopyrrolate
Aclidinium
4
Q
Cycloplegia + Mydriasis Musc Antagonist
A
Cyclopentolate
Tropicamide
5
Q
Bladder Incontinence Musc Antagonist
A
Oxybutynin Tolterodine Darifenacin Fesoterodine Solifenacen Trospium
6
Q
CNS (Parkinson’s) Musc Antagonist
A
Benztropine
Trihexyphenidyl
Biperiden
7
Q
Ipratropium
A
- Nonselective SHORT ACTING muscarinic receptor antagonist
- Deos NOT cross BBB
- Clinical: Bronchodilator (COPD/Acute Asthma); Rhinorhhea
- Minimal SE
8
Q
TioTropium
A
- Functionally Selective irreversibvle M3 Long acting Muscarinic Antagonist
- Does NOT cross BBB
- NO GI/RESP muscosa absorption; High Bronchial selectivity of action
- Clinical: CHRONIC management asthma/COPD; ONCE daily;
9
Q
Glycopyrrolate
A
- Nonselective w/ slight affinity for M3 LAMA
- Does NOT cross BBB
- Clinical: bronchospasm + COPD; Mucus secretions; Cerebral palsy drooling; Hyperhidrosis
- SE: Xerostomia, UTI
- Interactions: K+; Topiramate, Zonisamide (seizures)
10
Q
Aclidinium
A
- Selective M3 LAMA
- COPD
- Adverse: URI; Constipation; Cough; SOB; Glaucoma; UI Ret; Allergies
11
Q
Umeclidium
A
- Competitive Reversible Selective M# LAMA
- Maintenance treatment of COPD
- Same as Aclidinium for SE
12
Q
Cyclopentolate
A
- Selective M3 Musc agonist
- Cycloplegia for ALL ages
- Clinical: Diagnostic for Mydriasis and Cycloplegia; Short DOA
- AE: Irritation, lacrimation, INC Ocular pressure; drowsiness; ataxia; restlessness; visual hallucinations
13
Q
Tropicamide
A
- Selective M3 antagonist
- Shorter DOA 4-6 Hours
- Clinical: Diagnostic for Mydriasis/Cycloplegia
14
Q
Oxybutynin
A
- Competitive M3 Antagonist
- Clinical: Overactive Bladder including w/ neurological symptoms like Spina Bifida
- Met by CYP3A4
- Transdermal patch
15
Q
Other Overactive bladder Drugs
A
Tolterodine
Darifenacin
Fesoterodine: Prodrug; 5-HMT responsible for activity
Solifenacin: Children/adolescence w/ incontrinence
Trospium: Quaternary, but minimally crosses BBB
