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194 Cards in this Set
- Front
- Back
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Phosphodiesterase inhibitors (4)
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theophylline, caffeine, papverine, sildenafil
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Theophylline, Caffiene, Papverine
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prevents PDase from degrading cAMP, makes effects of epi last longer!!!
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Sildenafil MOA
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prevents PDase from degrading cGMP to 5'-GMP,
smooth muscle relaxation allows blood to fill corpus cavernosa |
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Sildenafil treats...
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impotence,
It's viagra! |
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PDase inhibitor that can be used as bronchodilaotr:
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theophylline, caffiene
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Theophylline adverse effects
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seizures, fatal arrhythmias
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(+) CYP450
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phenobarbital, rifampin, phenytoin, carbamazepine, ethanol (chronic), cigarrete, dixin, DDT, polychlorinated biphenyls
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(-) CYP450
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isoniazid, cimetidine, grapefruit, erythromycin, acute ethanol, ketoconazole
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Slow acetylators develop toxicity with:
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SHIP
sulfapyridine hydralazine isoniazid procainamide |
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Drugs that can cause lupus like syndrome
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procainamide, hydralazine
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Make urine acidic to increase excretion of weak bases (amphetamines)
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ammonium chloride
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make urine alkaline to increase excretion of weak acids (aspirin)
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acetazolamide
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Botlinum Toxin MOA
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hydrolyzes proteins involved in synaptic storage and exocytotic release of AcH, no transmission at NMJ
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Botulinum toxin treats:
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blepharospasm, stabismus, cervical dystonia, spasmodic torticollis, laryngeal dystonia, hemifacial spasm, myofacial pain syndrome
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ACh MOA
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muscarinic receptor agonist
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ACh Pharm affects
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rapid/transient decrease in BP, baroreflex tachycardia
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ACh uses
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Not many, b/c so many systemic affects.
rapid/complete miosis before/after eye surgery |
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Carachol/Carbamylcholine MOA
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Nicotinic and Muscarinic Agonist
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Carbachol/Carbamylcholine Pharm effects
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slow onset miosis
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Methacoline MOA/Uses
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Musarinic agonist, provocative agent in asthma diagnosis
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Bethanechol MOA
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Mucarinic agonist, selective GI/GU effects
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Bethanechol Pharm effects
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increased acid, motility, tone
relaxed sphincters, increased GI secretions, contract detrusor ***Low bioavailability |
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Bethanechol therapeutic uses
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bowel stasis, post-op bowel wake-up, make pee
-Helps you go number 1 and 2! |
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Bethanecol contraindication
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asthma, copd, peptic ulcer, CHF, hyperthyroidism.
It's a muscarinic agonist, so it turns up parasympathetics...bad if you have asthma/ulcers |
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Succinylcholine MOA
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IV- acts on N2 cholinergic receptors at NMJ
single contraction followed by flaccid paralysis (depoarization bloackade) |
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Succinylcholine degraded by
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plasmacholinesterase, fast- most degraded before it reaches the NMJ, not degraded by AChase, effect terminated by diffusing away
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Pilcarpine MOA
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selective Muscarinic agonist, not metabolized by AChase or pseudoAChase.
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Pilocarpine effects
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contraction of meridoninal fibers of ciliary muscle,
increases aqueous humor flow |
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Pilocarpine uses
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1st drug to treat glaucoma
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Pilocarpine adverse effects
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impaired far vision, persistant miosis (poor night vision)
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Pilocarpine contraindication
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asthma/COPD- bronchoconstriction
Peptic ulcer-- more acid hyperthyroid- atrial flutter/fib dilated heart- atrial flutter/fib |
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Cevimeline MOA/effects
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synthetic muscarinic agonist/increased salivation
treats dry mouth/dry eyes |
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Cholinergic agonist suffixes
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-ine, chol
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Cevimeline side effects
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GI cramps, sweating, UTH, rhinitis
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Drugs for glaucoma
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pilocarpine, betaxolol, timilol, lantanoprost/bimatoprost, epinepherine, dipivefrin, apraclonidine, acetazolaminde, dorzolaminde, isoflurophate (DFP), Echothiophate, Mannitol
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Drugs for acute angle-closure glaucoma
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mannitol, acetazolamide, pilocarpine
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betaxalol MOA
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selective B1 anatgonist, decreases production of aqueous humor
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timolol MOA
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B antagonist, decreases production of aqueous humor
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Latanoprost/Bimatoprost MOA
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Stable analog of PGF2alpha, increases uveoscleral outflow
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Epinepherine
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A1 agonist, enhance outflow of aqueous humor through normal pathway, causes mydriasis
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Dipiverfrin
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A1 agonist, hydrolyzed to EPI, enhances outflow of aqueous humor, causes mydriasis
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Apraclonidine
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A2 agonist, decreases production of aqueous humor, prevents postsurgical ocular hypertension
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Acetazolamide
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carbonic anhydrase inhibitor, stops aqueous humor production
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Dorzolamide
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carbonic anhydrase inhibitor, decreases production of aqueous humor, acetazolamide is better
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Isoflurophate (DFP)
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OP AChase inhibitor, increases amount of ACh available to contract the ciliary muscle
Topical |
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Echothiphate
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OP AChase inhibitor, increases amount of ACh available to contract the ciliary muscle
Topical |
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Mannitol
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Osmotic diuretic agent, hyperosmolar ECF causes cellular dehydration
for acute attacks |
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Drugs that decrease aqueous humor production
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carbonic anhydrase inhibitors, B antagonists, A2 agonists
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Drugs that increase normal outfolw
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A1 agonist, muscarinic agonist (pilocarpine) Achase inhibitor (isofluophate)
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Drugs that increase uv-scl outflow
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PGF2alpha analogs (latanoprost)
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Carbamate AChase inhibitors
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physostigimine, donepezil, neostigmine, pryidostigmine, erdrophonium, carbaryl
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physostigimine
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tertiatry, non-competitive, slowly reversible inhibition of AChase
no direct affect at AChase |
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physostigimine pharm effects/uses
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inhibits AChase, so ACh acts longer, not used much bc of side effects, alzheimer's but there are better drugs, OD w/ anticholinergics
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Donepezil MOA
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carbamate, reversible inhibitor of ACh, ACh will stay around longer
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Donepezil uses
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DOC for alzheimers b/c more selective for CNS, decreases apathy, anxiety, hallucinations & behavioral problems
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Donepezil S/E
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increased parasympathetics:
diarrhea, muscle cramps, fatigue, bradycardia, insomnia, anorexia |
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Neostigmine
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quaternary amine, direct agonst at N2 receptor, inhibits AChase @ all peripheral sites
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Neostigmine uses
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post-op bowel paralysis, GI/GU atony, myasthenia gravis, reversal of muscle paralysis caused by competitive NM blocks
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Pyridostigimine
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po, actis like neostigmine,
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prydiostigmine uses
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long term dosing for Myasthenia Gravis, po dose, quarternary No CNS affects
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Mild ocular myasthenia gravis treatment
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pyridostigmine + corticosteroids
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mild/moderate general myasthenia gravis sympotms
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pyridostigmine + thymectomy
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moderate/sever myasthenia gravis treatment
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pyridostigmine + azathioprine
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Edrophonium MOA
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quaternary carbamate AChase inbibitor. most action at NMJ from direct stimulation of N2 receptors
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Erdophonium is given
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IM or IV, can't use for home treatment of Myasthenia gravis
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Erdophonium therapeutic uses
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distinguish between myasthenic or cholinergic crisis. Too little or too much medication
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Give erdophonium with
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atropine to reverse competitive neruomusclar blockade caused by drugs
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S/E of ACHase inhibitors @ muscarinic sites
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excess salivation, rhinitis, bradycardia, bronchospasm, pooping, vomiting/diarrhea, urinary incontinence (all parasympathetic stuff)
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Carbaryl MOA
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IRREVERSIBLE AChase inhbitor. often grouped with OP poising because similar effects
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Treat carbaryl poisoning with
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atropine to block muscarinic stimulation, supportive care. Must resynthesize AChase.
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Organophosphate AChase inhibiors
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"DIP ME"
Dimpylmate Isofluorophate (DFP) Parathion Malathion Echothiphate |
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OP MOA
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phosphylates active site of ACHase
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Isofluophate and Echothiophate can be...
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given topically for glaucoma, increase ACh available for contraction of ciliary muscle. LAST RESORT: catarcts/toxicity
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Parathion is converted
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to active metaboolite paraoxon by CYP450
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Malathion is toxic to bugs but not birds and mammals because
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they have plasma carboxyesterases that destroy malathion.
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CNS symptoms of OP poisoning
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slow:
loss of concentration irritability forgetfulness depression |
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PNS symptoms of OP poisoning
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muscarinic manifestations:
eye CV lungs GI glands GU Extra parasympathetic effects In nicotinic receptors: -skeletal muscle -sympathetic ganglia - |
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More severe signs of CNS OP poisoning
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restlessness, nightmares, ataxia, hypotension, insomnia, slurred speech, convulsions, respiratory depression
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Treatment of OP poisoning
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Atropine sulfate: tertiary, blocks peripheral¢ral muscarinic receptors
Pralidoxime: quarternary, gets rid of OPs to send AChase back to normal) not used for cabamate poisoning because it does NOT increase rate of hydrolysis. |
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Atropine MOA
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tertiary muscarinic antagonist
blocks action of ACh at muscarinic receptors. |
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Atropine Pharm effects
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depends on dose.
Small dose --> Large glands-heart- bladder/bowel-eye |
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Atropine therapeutic uses, perioperative
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decreased production of saliva, counteract bradycardia caused by ocular pressure, visceral traction, carotid sinus stimulation, injection of multiple doses of succinyl choline
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Atropine as therapy in OP poisoning
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blocks stimulartion of muscarinics, decreases affect of the inhibition of ACHase
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Reverse neuromuscular blockade caused by drugs
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Atropine + Erdophonium
Erdophinum mostly acts at NMJ, atropine blocks muscarinics so all erdophium can stimulate NMJ |
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For determination of refractive error of lens and cataract surgery:
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Scopalamine, cyclopentolate, atropine
SAC -- mydriasis and cycloplegia |
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Atropine is DOC to relax sphincter/cilary muscle in
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anterior uveatis, choroidits, keratitis
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Atropine can reverse AV block induced by
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digoxin
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Atropine can revers bradycardia in children by
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increasing CO
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Atropine can prevent adverse affects of
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neostigmine and pyridostigmine in treatment of myasthenia gravis
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atropine can be given with _____to reduce abuse
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diphenoxylate--- habit forming diarrhea med, atropine gives bad S/E when doses are too big
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symtoms of atropine toxicity
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Red as a beet
Mad as a hatter dry as a desert hot as a pistol |
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Rx for atropine overdose
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gastric lavage, resp/circ support, sponge bath, foley, dark room, benzo for sedation
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CNS affects of atropine toxicity
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nervousness, excitation, confusion, hallucinations, weakness, giddiness, muscular incoordination, hypertension, maniacal tendencies.
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PNS affects of atropine toxicity
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dry mouth/thirst
hot, dry, flushed skin myadriasis/blurred vision tachycardia |
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Scopolamine
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tertiary muscarinic anatagonist with little effect on HR.
blocks muscarinics, but doesn't mess with HR much |
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Pharm affects of tertiary muscarinic receptor antagonists, general
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relax iris sphincter
relax cilary muscle (far vision) increase contractility in atria/ventricle Increased HR increased conduction velocity @ atria, decrease APD/ERP Decrease GI motility/tone relax GU tract/bronchi (smooth muscle) contracts sphincters decreased secretion from glands --All things that are good when running from a bear |
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therapeutic uses of scopalamine
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mydraiasis/cycloplegia (+ cyclpentolate & atropine)
DOC for pain in anterior eveitis, choroiditis, Keratitis motion sickness in patch used to be used as tranquilizer |
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Adverse effects of scopalamine
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CNS affects at therapeutic dose (unlike atropine)
-somonolence -euphoria, -amnesia -dreamless sleep -antegrade amnesia (worse with EtOH) |
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Cyclopentolate
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tertiary muscarinic antagonsit, DOC for refractive error.
SAC-- in the conjuncteval sac |
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Tropicamide MOA
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tertiary muscarinic antagonist @ Eye
'sundglasses in the tropics" |
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Tropicamide uses
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DOC for fundoscopic exam (short half-life)
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Benzotropine
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anatagonist at central muscarinic receptor
parkinson's treatment |
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Trihexyphenidyl
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antagonist at central muscarinic receptor
parkinson's treatment |
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Dicyclomine and Hyoscyamine
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muscarinic antagonists at GI tract, prevents bowel spasms with IBS
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Oxybutynin MOA/uses
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muscarinic antagonist, direct antispasmodic effect at detrusor
OAB |
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Oxybutynin adverse effects
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drowsiness, somnolence, dizziness
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Tolterodine uses/adverse effects
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OAB
dry mouth, blurred vision, constipation/somnolence |
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Solifenacin MOA/Uses/Adverse
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selective M3 atangonist
OAB fewer CNS effects: less dry mouth than other OAB drugs |
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Darifenacin MOA/Uses/Adverse
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Selective M3 antagonist
OAB No CNS/CV effects....less dry mouth than others! |
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Drugs for overactive bladder:
DOTTS |
Darifenacin, Ocybutynin, Toletrodine, Trospium (4), Solifenacin
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Diphenhydramine (benadryl)
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central muscarinic receptor antagonist/antihistamine
maybe used in parkinsons |
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Drugs used for Parkinsons
B-BAT |
Benztropine
Biperidin Atropine Trihexyphenidyl Benadryl (antihistamines/diphenyhydramine) |
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Side effects of drugs for parkinsons
C-CUD |
Cycloplegia (ciliary paralysis)
Constipation urinary retention dry mouth |
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Quarternary Muscarinic antagonist
N-methyl PIG |
N-methylatropine
N-methylhomatropine Methscopolamine Trospium Propantheline Ipratoprium Glycopyrrolate |
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quarternary drug used for OAB
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trospium, nonselective muscarinic antagonist, does NOT enter CNS
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Iprtropium MOA
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relaxes bronchial smooth muscle
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Glycopyrrolate MOA
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peripheral muscarinic antagonist,
prevents unwanted muscarinic stimulation from AChase inihition. |
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Glycopyrrolate perioperative uses
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decreased saliva and pulmonary secretion
counteract bradycardia caused by: ocular pressure, visceral traction, carotid sinus stimulation, multiple doses of succinylcholine |
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Glycopyrrolate + neostigmine
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given IV, reverses competitive neurmuscular blockade cause by drugs like (d-tubocurarine)
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Nicotine MOA
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direct stimulation of N1 and N2 cholinergic receptors
CNS: direct N1 stimulation releases NE/DA Addiction results from release of DA in nucleus acumbens |
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Compound in cigarette smoke that induces CYP-450
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Benzopyrene
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Actue CNS affects in a nicotene naive patient
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increased EEG alerting pattern
facilitation of attention&memory decrease aggression decrease appetit decrease skel muscle tone & DTR via stimulation of renshaw neurons, increase physiological tremor |
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Acute CV affectes in a nicotene naive patient
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increased SBP, DBP, PP, HR via stimulation of sympathetic ganglia & aortic chemoreceptors
tolerance develops rapidly, long term effects on BP aren't big decrease skin temp and digital BF (peripheral vasoconstriction) |
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Acute nicotine toxicity
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usually from chewing tobacco
-vomiting |
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Adverse effects of nicotine containing insecticides
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N/V, ab cramps, diarrhea
Salivation/sweating headache/disorientation/dizzy muscle weakness BP falls, HR irregular, shallow breathing, CV collapse, respiratory failure |
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Chronic nicotine toxicity
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increase LDL and TGs, lower HDL
decrease PGI2 and NO (constricted arterioles and platelet aggregation) neutrophil activation/aggregation--inflammatory damage cardiac dysrhythmias cancer (benzopyreme mutate p53) COPD/Asthma Smokers face--- wrinkles! |
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Pharm effects of chewing tobacco
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CV:
increased incidence of CV disease, HTN increased plasma insulin/fibrinogen Oral cancer: oral leukoplakia gum disease |
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Tx for nicotine toxicity
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gastric lavage or emesis
intubation drugs for shock/convulsions |
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Succinylcholine MOA
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IV causes single contraction at NMJ followed by 3-5 minutes of flaccid paralysis
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Succinylcholine pharm effects
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most dose degraded by plasmacholinesterase
partial repolarization, but NMJ block persists NMJ blockade is terminated by drug diffusing away |
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Trimethaphan MOA
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IV, competitive block of N1 receptors in autonomic ganglia, prevents all sympathetic and parasympathetic activity
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Mecamylamine MOA
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po, same as trimethaphan, blocks all parasympathetic and sympathetic stimulation
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effects of trimethaphan or mecamylamine due to sympathetic blockade
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arteriodilation - decreased TPR
venodilation- dec. preload dec dp/dt dec CO dec sweating impotence no ejaculation |
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effects of trimethaphan or mecamylamine due to parasympathetic blockade
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tachycardia
mydriasis&cycolplegia decreased salivation/lacrimation decreased GI fxn constipation/no pee no erection |
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therapeutic uses of trimethaphan
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controlled hypotension during head/neck surgery
causes histamine release so there is more vasodilation |
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mecamyliamine therapeutic uses
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autonomic hyperreflexia in pts with high spinal cord injuries (T5 and up)
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symptoms of autonomic hyperreflexia
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sudden onset with distention of
bladder. HTN, bradycardia (CBR), sweating, piloerection. |
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Direct adrenergic agonists
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NE, EPI, DA, dobutabine, isoproterenol, salmeterol, terbutaline, albuterol, pirbuterol, ritodrine
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NE MOA
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direct adrenergic agonist
a > B1 > B2 local, NOT circulating. vasoconstrict arterioles in kidneys, GI,skin (alpha) vasodilate liver/skeletal muscle (B2) |
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Therapeutic uses of of NE
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direct agonist: vasopressor agent when CO/tissue perfusion are normal (spinal shock)
vasoconstrictor with local anesthetics |
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NE adverse effects
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cardiac arrhythmias (B)
Angina in pts w/ CAD (B) Cerebrovascular hemorrhage (increased BP) pulmonary edema (increased TPR) Tremor (B2) |
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Epi MOA
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circulating hormone.
B2>B1>a |
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Epi pharm effects
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small/physio dose
B2 stimulation vasodilation in liver skeletal muscles large dose net vasoconstriction via alpha stim, increased TPR/DBP |
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Epi therapeutic uses
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DOC for anaphylactic shock, priapism
bronchodilator in asthma/COPD topical epi lowers IOP |
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Dopamine MOA
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adrenergic agonist
D1, B1, alpha |
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Pharm effects, small DA dose
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D1 stimulation- dilate renal afferent arterioles
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Pharm effects, medium DA dose
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D1 and B1 stimulation
increased dp/dt with little effect on HR, further increase in RBF bc of increase CO and contractility |
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Direct adrenergic agonists
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NE, EPI, DA, dobutabine, isoproterenol, salmeterol, terbutaline, albuterol, pirbuterol, ritodrine
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NE MOA
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direct adrenergic agonist
a > B1 > B2 local, NOT circulating. vasoconstrict arterioles in kidneys, GI,skin (alpha) vasodilate liver/skeletal muscle (B2) |
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Therapeutic uses of of NE
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direct agonist: vasopressor agent when CO/tissue perfusion are normal (spinal shock)
vasoconstrictor with local anesthetics |
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NE adverse effects
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cardiac arrhythmias (B)
Angina in pts w/ CAD (B) Cerebrovascular hemorrhage (increased BP) pulmonary edema (increased TPR) Tremor (B2) |
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Epi MOA
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circulating hormone.
B2>B1>a |
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Epi pharm effects
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small/physio dose
B2 stimulation vasodilation in liver skeletal muscles large dose net vasoconstriction via alpha stim, increased TPR/DBP |
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Epi therapeutic uses
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DOC for anaphylactic shock, priapism
bronchodilator in asthma/COPD topical epi lowers IOP |
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Dopamine MOA
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adrenergic agonist
D1, B1, alpha |
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Pharm effects, small DA dose
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D1 stimulation- dilate renal afferent arterioles
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Pharm effects, medium DA dose
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D1 and B1 stimulation
increased dp/dt with little effect on HR, further increase in RBF bc of increase CO and contractility |
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Pharm effects, large DA dose
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begins to stimulate alphas, decrease SV/CO
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therapeutic uses of DA
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increase CO post MI
inc BP in septic hemorrhagic shock inc in CO in CHF which is refractory to digoxin +diruetics. inc urine flow in treatment of barbituate&salicylate |
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Dobutamine MOA
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racemic mix stim both B1 > B2
(+) A1 agonist (-) A2 antagonist opposite alpha stimulations cancel each other out |
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Pharm effects of Doubutamine
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B1: inc SV
B2: arteriodilation - dec TPR venodilation- dec venous return increases GFR via inc in CO |
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Dobutamine >> dopamine in MI
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Dobutamine does NOT inc DBP
Dobutamine is LESS likely to cause tachycardia Dobutamine causes venodilation, dec venous return |
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Dobutamine adverse effects
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tachycardia, dysrhythmias, cardiac arrhythmias (B), Angina in pts w/ CAD (B), Tremor (B2)
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Isoproterenol MOA
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iv pure beta 1=2
like epi, but no a stim |
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Isoproterenol affects
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B1: inc dp/dt, inc HR, inc SV
B2: vasodilation, dec TPR inc AV conduction in AV block adverse: arrhythmias, angina in pts with CAD(B) Tremor (B2) tachycardia- worse than albuterol |
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Selective B2 agonists
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salmeterol, terbutaline, albuterol, pirbuterol, ritodrine
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Selective B2 agonist pharm effects
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relax smooth muscle-- bronchial for salmeterol, terbutaline, albuterol, pirbuterol
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Ritodrine
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selective B2 agonist used to uterus to delay birth or move baby from breech.
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Phenylephrine (PE)
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IV A1 agonist,
(NE effects) inc DPB, SBP SV unchanged, Dec HR (CBR) |
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Therapeutic uses of Phenylephrine
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systemic vasoconstictor, local app is a nasal decongestion,
mydriasis for fundoscopic exam |
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Oxymetazoline
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alpha agonist
nasal decongestant, longer duration that Phenylephrine |
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Tyramine
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in aged food
causes release of endogenous NE, inc BP |
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Ampethamine
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cause release of NE, blocks uptake, lipid soluble
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Ephedrine
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B1/B2 agonists
release of endogenous NE lipid soluble direct B/indirect alpha stim |
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Ephedrine pharm effect
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reverse hypotension from anesthisia,
bronchodilation, mydriasis, insomnia |
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Pseudophedrine
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same as ephedrine, but less effect, used as nasal decongesant
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Phenoxybenzamine
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noncompetitive alpha blocker. more A1 than A2
Dec TPR/BP, inc venous capacitance, inc HR, inc dp/dt No change in CO |
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Phentolamine
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A1=A2 block
dec TPR, inc venous capacitance, inc dp/dt no change in CO |
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Phenoxybenzamine uses
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control BP in pts with malignant tumors
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Phentolamine uses
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used perioperatively w/ nonselective B blocker to control BP during manipulation of Pheo
local use to reverse ischemia from DA impotence (local injection) |
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Adverse effects of phenoxybenzamine and phentolamine
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angina, tachycardia, miosis (A1), inhib of ejaculation, inc insulin resistance
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Prazosin (terazosin, doxazosin)
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only alpha1 blocker
decr TPR/BP inc venous capacitnce no change HR, dp/dt&CO |
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Prazosin uses
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first line HTN
used with nonselective B-blocker in Pheo treatment of frostbite small dose can relieve uriniary obstruction in BPH |
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Tamsulosin
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A1a block, DOC for BPH
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Labetolol
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A1/B1 block
Dec TPR, DP, dp/dt no change in HR/CO first line in HTN |
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Yohimbine
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A2 >>A1, very lipid-soluble
central A2 blockade in baroreflex arc, increases pregang sympathetic nerve |
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Ergotamine and Dihydroergotamine
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partial alpha agonist, slight cerebral vessel constriction (migranes)
adverse: spontaneous abortion, muscle pain, paresthesias, digital vasospasm, gangrene miosis (a1) inhib of ejac (a1) inc insulin (a2) |
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alpha blocker possible side-effects
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orthostatic hypotension
failure to ejaculate miosis nasal congestion abdominal cramping some pt slowly retain Na/water to inc ECF volume |
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treatment of impotence
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phentolamine, papverine, sildenafil, alprostadil
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Phentolamine MOA
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inject into penis--ouch!,
competitive alpha blocker (1=2) |
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phentolamine pharm effects
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erection!
dec tpr/bp inc venous capcitance, HR, dp/dt Net: No change in CO |
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papaverine and sildenafil MOA
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PDEase inhibitor
for impotence |
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Alprostadil MOA
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topical or injected into corpus cavernosa
PGE1 analog |
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cardioselective b-blockers
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betaxolol, atenolol, metoprolol
B1 selective, cardio blocking only |
