Pharmacology Exam II

18 flashcards · Other · by Jared Blackwell

  1. M1 receptor

    CNS and Sympathetic postganlionic neurons. Primarily neural. M1 and M3 signal via IP3 and DAG.

  2. M2 receptor

    Heart: slows and decreases contractility. -Only muscarnic found on SA & AV nodes. Also non-vascular smooth muscle. M2 signals via opening K+ channel and inhibits adenylyl cyclase.

  3. M3 receptor

    Only muscarnic type on glands, and vascular smooth muscle. Eye: Contrict pupil, increase lacrimation. Endotheliuim: Release EDRF (not inv.) Vasodilate. GI tract & Bladder: Contract walls and relax sphicter, increase secretions. Thermoregulatory sweat, Erection, Contract uterus. M1 and M3 signal via IP3 and DAG

  4. Alpha 1 Adrenergic

    Generally causes contraction. -Contracts blood vessels, bladder, uterus, prostate, dilator muscle. -Dilates pupil, ejaculation.

  5. Alpha 2 Adrenergic

    Relax GI smooth muscle. Presynaptic parasympathetic nerve terminals - inhibition. "NO alpha 1, you SHALL NOT BE ACTIVATED" Inhibit lipolysis. Aggreate platelets.

  6. Beta 1 Adrenergic

    Increase rate and force of heart contraction.

  7. Beta 2 Adrenergic

    Relax brochial, uterine, & vascular smooth muscle. Inhibit labor. Activate glycogenolysisis in liver. Increase insulin.

  8. Beta 3 Adrenergic

    Increase lipolysis.

  9. Describe nicotine cholinergic receptor

    -Pentamer of polypeptide subunits. Located in postgang. neuron cell bodies in all ANS ganglia. NMJ. -In skeletal muscle, has two alpha 1, and one Beta 1, Epsilon, & Delta. Blocked by a-bungarotoxin & d-tubocuraine. -In ANS ganglia, has two alpha 3 and three Beta 4. Blocked by hexamethonium.

  10. Describe muscarinic cholinergic receptors

    Have M1-M5. All found in CNS. M1, 4, 5 neural. M2 SA & AV node. M3 glands. GPCR w/ 7 transmembrane helix. M1, 3, 5 are coupled with Gq - stimulates PLC --> DAG & IP3 --> Ca2+ release --> smooth muscle contract and gland secretion. -In vascular endothelial cells, Ca2+ leads to NOS --> smooth muscle relaxation. M2 & M4 are couple to Gi --> decrease cAMP and open K+ channels.

  11. What does AChE and PDE type 5 do?

    AChE and PDE 5 are both indirect cholinergic acting agonist. AChE elevates ACh in synapse. PDE 5 elevates cGMP in target cell.

  12. What are the three Cholinergic Agonists?

    -Choline esters -Plant alkaloids -Synthetic drugs

  13. Describe a choline ester

    One type of cholinergic agonist. Pos. charged quaternary amine compound. Poorly absorbed in gut. NO crossing BBB. Ex: ACh, carbachol, methacholine, & bethanocol. -These bind to nicotinic and muscarinic receptors except Bethanocol -only muscarinic. Overdose - "All faucets turned on"

  14. Acetylcholine use, mechanism of action, and toxicity.

    Choline ester of acetic acid. Rapidly metabolized by AChE, limits clinical use. Use: Ophthalmic solution produces miosis after cataract surgery. Angina give injection, M3 vascular smooth muscle cells, dilate.

  15. Carbachol, bethanechol, methacholine use, mechanism of action, and toxicity.

    Choline esters of carbamic acid. Direct Acting Cholinergic Stimulants Resistant to AChE, longer half-life. Carbachol used for miosis with topical application, M3. Bethanechol treats urinary retention, stimulates detrusor. (Muscarine specific). Methacholine diagnostic for asthma, asthamatics respond to lower dose. (Bronchoconstriction, muscous secretion).

  16. Alkaloids

    Direct Acting Cholinergic Stimulants. Tertiary Amines. "NICC SUCC MUSIC PILLS" Muscarine - NO clinical use. Binds better than ACh. NOT broken by AChE. Pilocarpine - Well absorbed topically or orally. Higher affinity for muscarinic than nicotine receptors. -Treats dry mouth and Glaucoma.

  17. Glaucoma

    Increase in IOP, build up of aqueous humor. Drain through trabecular meshwork. 1) Open angle - clogged trabecular. Treat with muscarinic agonists, Pilocarpine, ciliary muscles contract, opening trabecular meshwork. -Also treat with B-adrenergic antaognist and a-2 agonist. Decrease aqueous humor. 2) Closed angle - Iris blocks canal. Rapid onset.

  18. Synthetic drugs for cholinergic receptors

    Cevimeline treats xerostomia associated with radiation therapy of head/neck. Stimulates saliva making it easier to speak. -Adverse sweating, visual disturbances due to miosis.