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111 Cards in this Set
- Front
- Back
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Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
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Severe hypertension
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Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
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Ethanol
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Reversal of blockade by neuromuscular blockers
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Cholinesterase inhibitors
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Pneumonic for beta receptors
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You have 1 heart (Beta 1) and 2 lungs (Beta 2)
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Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
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Nondepolarizing Neuromuscular Blockers
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Agent with zero-order kinetics
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Ethanol
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Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short duration of action
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Succinylcholine
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This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
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Bethanechol
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Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
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Cholinesterase regenerators, pralidoxime
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Rate limiting step of alcohol metabolism
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Aldehyde dehydrogenase
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Used to treat patients exposed to insecticides such as parathion
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Pralidoxime, atropine
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This is the drug of choice for anaphylactic shock
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Epinephrine
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System that increases in activity with chronic exposure and may contribute to tolerance
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MEOS
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Prototypical drug is atropine
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Nonselective Muscarinic Antagonists
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Agent that metabolize acetaldehyde to acetate
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Aldehyde dehydrogenase
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Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
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Amphetamines
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Agents that inhibit acetaldehyde dehydrogenase
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Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
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Only direct acting agent that is very lipid soluble and used in glaucoma
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Pilocarpine
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Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
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Disulfiram
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Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
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Phenylephrine
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The most common neurologic abnormality in chronic alcoholics
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Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
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Time it takes for amount of drug to fall to half of its value; this is a constant in first order kinetics (majority of drugs)
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Half-life (T1/2)
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Agent that is teratogen and causes a fetal syndrome
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Ethanol
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Newer alpha 2 agonist (apraclonidine and brimonidine) treat glaucoma by acting to
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Reduce aqueous secretion
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Agent that is the antidote for methanol overdose
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Ethanol, fomepizole
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This agent used to treat dry mouth in Sjögren's syndrome
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Cevimeline
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Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
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Fomepizole
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Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis
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Albuterol
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Agent that inhibits alcohol dehydrogenase and its clinical use
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FOMEPIZOLE – used to prevent formation of toxic metabolites from methanol and ethylene glycol ingestion
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Treat manifestations of Parkinson's disease and EPS
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Benztropine, trihexyphenidyl
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Longer acting Beta 2 agonist is recommended for prophylaxis of asthma
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Salmeterol
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Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
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Edrophonium
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These agents increase cardiac output and may be beneficial in treatment of acute heart failure and some types of shock
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Beta1 agonists
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Antidote used for lead poisoning
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Dimercaprol, EDTA
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These agents decrease blood flow or increase blood pressure, are local decongestants, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
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Alpha1 agonists
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Carbamate with intermediate action, used for+A1170 postoperative and neurogenic ileus and urinary retention
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Neostigmine
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Shock due to septicemia or myocardial infarction is made worse by
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Increasing afterload and tissue perfusion declines
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Treatment of motion sickness
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Scopolamine, meclizine
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Epinephrine is often mixed with a local anesthetic to
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Reduce the loss from area of injection
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Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
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Physostigmine
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Chronic orthostatic hypotension can be treated with
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Midodrine
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Relates the amount of drug in the body to the plasma concentration
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Volume of distribution (VD)
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Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
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Terbutaline
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Treatment of myasthenia gravis
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Pyridostigmine
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Sympathetic agent which stimulates heart rate and can dilate vessels in skeletal muscle at low doses
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Epinephrine
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Produce mydriasis and cycloplegia
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Atropine, homatropine,C1208 tropicamide
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Mast cells to reduce release of histamine and inflammatory mediators
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Epinephrine
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Antiglaucoma organophosphate
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Echothiophate
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Agent used in shock because it dilates coronary arteries and increases renal blood flow
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Dopamine
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Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis
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Phenoxybenzamine
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Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
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Dobutamine
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Associated with an increased incidence of cataracts in patients treated for glaucoma
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Long acting cholinesterase inhibitors
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Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
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Ephedrine
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Bronchodilation in asthma and COPD
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Ipratropium
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Alpha 1 agonist toxicity
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Hypertension
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Scabicide organophosphate
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Malathion
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Beta 1 agonist toxicity
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Sinus tachycardia and serious arrhythmias
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Plasma concentration of a drug at a given time
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Cp
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Beta 2 agonist toxicity
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Skeletal muscle tremor, tachycardia
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Organophosphate anthelmintic agent with long DOA
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Metrifonate
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The selective agents loose their selectivity at
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high doses
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Reduce transient hyper GI motility
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Dicyclomine, methscopolamine
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Toxicity of organophosphate:
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DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
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Antidote used for cyanide poisoning
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Nitrites
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The most frequent cause of acute deaths in cholinesterase inhibitor toxicity
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Respiratory failure
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Cystitis, postoperative bladder spasms, or incontinence
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Oxybutynin, dicyclomine
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The most toxic organophosphate
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Parathion
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The ratio of the rate of elimination of a drug to its plasma concentration
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Clearance (CL)
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Treatment of choice for organophosphate overdose
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Atropine
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Toxicity of anticholinergics
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block SLUD (salivation, lacrimation, urination, defecation
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This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
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Pralidoxime
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Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena
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Phentolamine
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Another pneumonic for anticholinergic toxicity
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"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
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The elimination of drug that occurs before it reaches the systemic circulation
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First pass effect
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Atropine fever is the most dangerous effect and can be lethal in this population group
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Infants
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Antidote used for anticholinergic poisoning
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Physostigmine
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Contraindications to use of atropine
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Infants, closed angle glaucoma, prostatic hypertrophy
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The fraction of administered dose of a drug that reaches systemic circulation
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Bioavailability (F)
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Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
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Prazosin, terazosin, doxazosin
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When the rate of drug input equals the rate of drug elimination
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Steady state
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Antidote used for organophosphate/anticholinesterase poisoning
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Atropine, pralidoxime (2-PAM)
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This step of metabolism makes a drug more hydrophilic and hence augments elimination
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Phase I
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Selective Alpha-1A blocker, used for BPH, but with little effect on HTN
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Tamsulosin
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Different steps of Phase I
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Oxidation, reduction, hydrolysis
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Antidote used for iron salt toxicity
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Deferoxamine
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Inducers of Cytochrome P450 (CYP450)
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Barbiturates, phenytoin, carbamazepine, and rifampin
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Selective Alpha 2 blocker used for impotence (controversial effectiveness)
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Yohimbine
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Inhibitors of CYP450
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Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine (Mucomyst)
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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
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Antidote for arsenic, mercury, lead, and gold poisoning
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Dimercaprol
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Type of kinetics when a constant percentage of substrate is metabolized per unit time
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First order kinetics
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
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Penicillamine
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Drug elimination with a constant amount metabolized regardless of drug concentration
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Zero order kinetics
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Antidote used for heparin overdose
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Protamine
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Target plasma concentration times (volume of distribution divided by bioavailability)
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Loading dose (Cp*(Vd/F))
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Physical properties
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Properties which can be observed without changing the substance into something different. Color; odor
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Concentration in the plasma times (clearance divided by bioavailability)
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Maintenance dose (Cp*(CL/F))
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid
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Antidote used for methanol and ethylene glycol
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Ethanol or fomepizole
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Antidote used for opioid toxicity
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Naloxone (IV), naltrexone (PO)
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Antidote used for benzodiazepine toxicity
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Flumazenil
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Antidote used for tricyclic antidepressants (TCA)
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Sodium bicarbonate
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Antidote used for carbon monoxide poisoning
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100% O2 and hyperbaric O2
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Antidote used for digitalis toxicity
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Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
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Antidote used for beta agonist toxicity (eg. Metaproterenol)
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Esmolol
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Antidote for methotrexate toxicity
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Leucovorin
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Antidote for beta-blockers and hypoglycemia
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Glucagon
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Antidote useful for some drug induced Torsade de pointes
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Magnesium sulfate
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Antidote for hyperkalemia
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sodium polystyrene sulfonate (Kayexalate)
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Antidote for salicylate intoxication
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Alkalinize urine, dialysis
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