Intro Pharm Flashcards
Alpha1 receptors
Sympathetic
Linked with Gq proteins
1) Increase vascular smooth muscle contraction
2) Increase pupillary dilator muscle contraction (mydriasis)
3) Increase intestinal and bladder sphincter muscle contraction
Alpha2 receptors
Sympathetic
Linked with Gi proteins
1) Lower sympathetic outflow
2) Lower insulin release
3) Lower lipolysis
4) Increase platelet aggregation
5) Lower aqueous humor production
B1 receptors
Sympathetic
Linked with Gs proteins
1) Increase HR
2) Increase Contractility
3) Increase renin release
4) Increase Lipolysis
B2 receptors
Sympathetic
Linked with Gs proteins
1) Vasodilation
2) Bronchodilation
3) Increase lipolysis
4) Increase insulin release
5) Lower uterine tone (tocolysis)
6) Ciliary muscle relaxation
7) Increase aqueous humor production
M1 receptors
Parasympathetic
Linked with Gq proteins
1) CNS
2) Enteric Nervous System
M2 receptors
Parasympathetic
Linked with Gi proteins
1) Lower HR
2) Lower contractility of atria
M3 receptors
Parasympathetic
Linked with Gq proteins
1) Increase exocrine gland secretions (lacrimal, salivary, gastric acid)
2) Increase gut peristalsis
3) Increase bladder contraction
4) Increase bronchoconstriction
5) Increase pupillary sphincter muscle contraction (miosis)
6) Increase ciliary muscle contraction (accommodation)
D1 receptor
Dopamine
Linked with Gs proteins
Relaxes renal vascular smooth muscle
D2 receptor
Dopamine
Linked with Gi proteins
Modulates transmitter release, esp in brain
H1 receptor
Histamine
Linked with Gq proteins
1) Increased nasal and bronchial mucus production
2) Increased vascular permeability, contraction of bronchioles, pruritis, and pain
H2 receptor
Histamine
Linked with Gs proteins
Increases gastric acid secretion
V1 receptor
Vasopressin
Linked with Gq proteins
Increase vascular smooth muscle contraction
V2 receptor
Vasopressin
Linked with Gs proteins
Increase H2O permeability and reabsorption in collecting tubules of kidney.
Bethanechol
Cholinomimetic Direct Muscarinic Agonist
Use: Postoperative ileus, neurogenic ileus, urinary retention
Activates bowel and bladder smooth muscle; resistant to AChE
Carbachol
Cholinomimetic - Direct Muscarinic agonist
Use: Constricts pupil and relieves intraocular pressure in glaucoma
Carbon copy of acetylcholine
Methacholine
Cholinomimetic - Direct Muscarinic agonist
Use: Challenge test for diagnosis of asthma
Stimulates muscarinic receptors in airway when inhaled
Pilocarpine
Cholinomimetic - Direct Muscarinic agonist
Use: Potent stimulator of sweat, tears, and saliva. Open angle and close-angle glaucoma
Contracts ciliary muscle of eye (open-angle glaucoma), pupillary sphincter (closed-angle glaucoma); resistant to AChE
Donepezil
Galantamine
Rivastigmine
Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase
Use: Alzheimer
Increase ACh
Edrophonium
Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase
Use: Historically, diagnosis of myasthenia gravis (extremely short acting). Myasthenia now diagnosed by anti-AChR Ab (anti-acetylcholine receptor antibody) test.
Increases ACh
Neostigmine
Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase
Use: Postop and neurogenic ileus and urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade (postop)
Increases ACh
No CNS penetration
Physostigmine
Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase
Use: Anticholinergic toxicity; crosses BBB into CNS
Increases ACh
For Atropine overdose
Pyridostigmine
Cholinomimetic - Indirect muscarinic agonist/ anticholinesterase
Use: Myasthenia gravis (long acting); does not penetrate CNS
Increases ACh
Increases muscle strength
Cholinomimetic (Muscarinic agonist) cautions
For all of these agents, look out for exacerbation of COPD, asthma, and peptic ulcers when giving to susceptible patients.