Midterm 1 Flashcards
Pilocarpine
Selective muscarinic agonist.
Treats glaucoma by causing the contraction of ciliary muscles (M3 receptor) and increase in aqueous humor drainage.
Bethanechol
Selective muscarinic agonist (synthetic analogue).
Used to increase GI motility and bladder tone after surgery.
Atropine
Competitive muscarinic antagonist.
Used to dilate pupil, treat slow heart rate, and reduce secretion during surgery.
Ipratropium bromide
Competative muscarininc antagonist (synthetic analogue).
Treats asthma and COPD by dilating bronchi.
Muscarinic Agonists treat…
- Glaucoma
- Dry mouth
- Stimulate tone in bladder after surgery
- Increase gut motility
Side effects of muscarinic agonists…
Stimulates all muscarinic receptors, GI disturbances (nausea and vomiting), CNS effects, bradycardia, salivation and bronchoconstriction.
Nicotinic agonist uses and side effects
Used to treat nicotine addiction (patch, gum, aerosol). Side effects (CNS): tremor, convulsions, coma
Curare
Nicotinic antagonist - non-depolarizing (competative) antagonist.
You can overcome blockade by increasing ACh with AChE inhibitor.
Used to produce skeletal muscle paralysis during surgery and in ICU.
Side effects: paralysis
Succinylcholine
Nicotinic antagonist - depolarizing (non-competative) antagonist.
You cannot overcome blockade by increasing ACh with AChE inhibitor.
Used to produce skeletal muscle paralysis during surgery and in ICU.
Neostigmine, physostigmine
Indirect acting cholinergic agent.
Inhibits metabolism of ACh in synapse (increases ACh duration).
Reversible cholinesterase inhibitor (weakly binds).
Uses: increases gut and bladder motility, treats glaucoma, treats myasthenia gravis.
Side effects: salivation, miosis, bronchoconstriction, bradycardia, nausea.
Insecticides (melathion) and nerve gases (sarin)
Irreversible cholinesterase inhibitor (covalent bond with AChE)
Effects at both muscarinic and nicotinic receptors.
Initial signs muscarinic (bronchoconstriction, salivation, GI symptoms, CNS symptoms). Followed byt CNS and PNS nicotinic signs (activation of skeletal muscle, paralysis).
Treatment: support respiration, decontamination, use muscarinic antagonist (atropine) and a compund that can break the covalent bond with the inhibitor (pralidoxime).
Differences between the 3 types of muscle.
Smooth: single nucleus, non striated, in walls of vessels and hollow organs, involuntary.
Cardiac: striated, single nucleus, branched, involuntary.
Skeletal: striated, multi nucleated, voluntary.
Types of receptors on presynaptic symp nerves, smooth muscles, heart, and other
Symp nerves: alpha 2
Smooth muscle: alpha 1 and beta 2
Heart: Beta 1
Other: alpha 2 and beta 2
Phenylephrine
Direct adrenergic alpha 1 agonist.
Treats: Nasal congestion (constricts bvs in nasal mucosa), dilates pupils (activates alpha 1 receptors), combines with local anesthetic (constricts bvs and prolongs nerve block).
Side effects: can increase BP
Clonidine
Direct adrenergic alpha 2 agonist.
Decreases release of NE via inhibition of AC and cAMP signalling.
Treats: hypertension
Side effects: sedation