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Pharm Test 2 drugs
Synaptic TM, Adrenergic, Cholinergic Agonists and Antagonists, Serotonin, Dopamine, NM relaxants, Opioid analgesics, Local and General anesthetics, NSAIDs
116
Pharmacology
Professional
08/25/2013

Additional Pharmacology Flashcards

 


 

Cards

Term
Metyrosine
Definition

Indications: HTN

 

MOA: Competitive inhibition of tyrosine hydroxylase - decreases levels of DA and NE

 

 

PATHWAY: Tyr-->DOPA-->dopamine-->NE-->epinephrine

Term
Reserpine
Definition

Indications: HTN

 

MOA: inhibits VMAT uptake of monoamines - leaves monoamines susceptible to degradation by MAO

 

Adverse effects: not only prevents dopamine from getting into vesicles, it also prevents serotonin, NE, epi.. people were getting depressed so they took it off the market and later reintroduced it at lower doses

Term
Bretylium
Definition

Indications: Ventricular arrhthymia

 

MOA: inhibits AP generation and calcium dependent synaptic vesicle fusion - hyperpolarizes membrane of the neuron. Bretylium has affinity for, and is taken up by reuptake transporters proteins that normally take up NE.

Term
Cocaine
Definition

Indications: analgesia in surgery

 

MOA: blocks monoamine reuptake

 

Adverse effects: you might become a coke wh*re


Other: Reuptake inhibitor drugs are highly effective because reuptake is the MAIN way that adrenergic neurotransmission is ceased

Term
Naloxone, Naltrexone
Definition

Indications: opioid overdose (Naloxone) or dependence as well as alcoholism (Naltrexone)

 

MOA: Non-peptide blockers of opioid receptors in CNS

Term
SSRIs
Definition

Indications: depression/anxiety

 

MOA: selective inhibition of serotonin reuptake transporter

Term
ACE inhibitors (eg. lisinopril)
Definition

Indications: HTN

 

MOA: inhibits peptide cleavage of AT I to AT II (a potent vasoconstrictor)

 

Adverse effects: dizziness, irregular heartbeats

Term
Monoamine oxidase (MAO) inhibitors
Definition

Indications: depression

 

MOA: blockade of cytoplasmic metabolism of monoamines

 

Contraindications: tyramine in cheeses, chianti = hypertensive crisis, merperidine, triptan

Term
L-DOPA
Definition

Indications: Parkinson's Disease

 

MOA: Precursor of dopamine, stimulates dopamine production

 

Adverse effects: cardiovascular system due to enhanced NE neurotransmission in the peripheral autonomic nerves 

Term
Carbidopa
Definition

Indications: Parkinson's Disease

 

MOA: Blocks L-DOPA conversion to dopamine, does not cross BBB, so protects peripheral adrenergic neurons from producing too much dopamine and NE when taking L-DOPA

 

Term
Tyramine
Definition

Indications: not therapeutic - ingested in diet

 

MOA: competes with NE for transport into synaptic vesicle

 

Contraindications: MAO inhibitors

Term
Tricyclic Antidepressants (TCAs)
Definition

Indications: depression

 

MOA: blocks monoamine reuptake

 

Adverse effects: depleting NE from use in cardiovascular system 

Term
Botulinum Toxin
Definition

Indications: cosmetic purposes, diplopia, paralysis of overactive muscles

 

MOA: prevents calcium dependent exocytosis of NT by inhibiting SNARE docking for vesicular release

 

Adverse effects: muscle weakness, trouble swallowing

 

Other: Botulinum Toxin can only get into CHOLINERGIC neurons

Term
Epinephrine
Definition

Indications: anaphylaxis, shock, cardiac arrest, heart block, bronchospasm

 

MOA: alpha and beta agonist -- at low conc, B2 receptor causes peripheral vasodilation and decreases DIASTOLIC BP (but systolic pressure still increases)and B1 receptor has pos inotropic and chronotropic effects, increasing systolic BP. At higher doses, a1 receptor activation predominates (= peripheral vasoconstriction and elevated diastolic pressure). B2 receptor causes bronchodilation and a1 causes dec in bronchiole secretions.

 

Adverse effects: arrhythmias, cerebral hemorrhage, anxiety, cold extremities, pulmonary edema


Contraindications: late term pregnancy due to unpredictable effects on fetal blood flow

 

Other: short acing due to susceptibility to degradation; B-receptor effects predominate at low concentrations

Term
Norepinephrine
Definition

Indications: acute hypotension due to vasodilatory shock


MOA: alpha-agonist, beta1-agonist; a1 causes peripheral vasoconstriction (inc TPR and diastolic BP), B1 causes increased systolic BP. Overall inc in MAP. Reflex baroreceptor response will cause a DECREASE in HR.

 

Adverse effects: arrhythmias, ischemia, HTN

 

Contraindications: pre-existing excessive vasoconstriction and ischemia and late term pregnancy

 

Other: NE has limited affinity for B2 receptors

 

REMEMBER NE CAUSES A REFLEX BRADYCARDIA

Term
Dopamine
Definition

Indications: CARDIOGENIC SHOCK

 

MOA: stimulates D1 receptors at low conc (decreases TPR), stimulates B1 receptors at medium conc (increases contractility and HR), stimulates a-receptors at higher infusion rates (increases BP and TPR)

 

Adverse effects: low infusion rates - hypotension; high infusion rates-ischemia

 

Contraindications: uncorrected tachyarrhythmias or ventricular fibrillation

 

Other: advantageous during cardiogenic shock due to vasodilatory effect in renal and mesenteric vascular beds

Term
Isoproterenol
Definition

Indications: BRONCHOSPASM (during anesthesia or bradycardia), transient heart block if TPR is high

 

MOA: non-selective B-agonist; B2 promotes peripheral vasodilation, decreased diastolic BP; B1 - positive inotropy and chronotropy = TRANSIENT increased systolic BP that is overcome by vasodilatory effect (overall small decrease in MAP). Reflex HR INCREASE. Bronchodilation.

 

Adverse effects: tachyarrhythmias

 

Contraindications: angina, particularly with arrhythmias REMEMBER ISO CAUSES A REFLEX TACHY WITH WIDENED PULSE PRESSURE

Term
Dobutamine
Definition

Indications: Short term Rx for low cardiac contractility in CHF, cardiogenic shock or excess B-blockade

 

MOA: selective B1-agonist; increased CO, positive inotropic effect > positive chronotropic effect due to lack of B2-mediated vasocilation and reflex tachycardia [BUT at higher doses, it may act as a B2 agonist and cause hypotension with reflex tachycardia]

 

Adverse effects: arrhythmias, hypotension (high doses), hypertension (low doses)

 

Contraindications: subaortic stenosis

 

Other: it is rapidly degraded by COMT

Term
Terbutaline
Definition

Indications: Prevent and reverse bronchospasm in asthma, bronchitis and emphysema

 

MOA: B2-agonist

 

Adverse effects: tachycardia, tolerance, skeletal muscle tremor (by activation of B2 receptors expressed on pre-synaptic nerve terminals of cholinergic somatomotor neurons) 

Term
Albuterol
Definition

Indications: Bronchial SM relaxation

 

MOA: B2-agonist

 

Adverse effects: tachycardia, tolerance, skeletal muscle tremor (by activation of B2 receptors expressed on pre-synaptic nerve terminals of cholinergic somatomotor neurons) 

Term
Phenylephrine
Definition

Indications: Pressor agent for anesthesia or shock, nasal decongestant, dilate pupil for eye exam (mydriatic agent), paroxysmal supraventricular tachycardia

 

MOA: selective a1-agonist; peripheral vasoconstriction and increased BP, activates baroreceptor reflex and decreases HR; decreases bronchial and upper airway secretions

 

Adverse effects: hypertension

 

Contraindications: hypertension

 

Other: Phenylephrine is not a catecholamine and therefore is not subject to rapid degradation by COMT. It has a much longer duration of action.

Term
Clonidine
Definition

Indications: HTN when cause is due to excess sympathetic drive

 

MOA: selective a2-agonist; peripheral vasoconstriction; crosses BBB to cause reduced sympathetic outflow and REDUCES vasoconstriction and BP = OVERALL reduction in BP; reduces the tonic excitatory input to sympathetic cells which reduces sympathetic output to vascular SM

 

Adverse effects: dry mouth, withdrawal after chronic use can result in life-threatening hypertensive crisis

Term
Amphetamine/Methamphetamine
Definition

Indications: Narcolepsy, ADHD

 

MOA: INDIRECT SYMPATHOMIMETIC - cause release of NE from adrenergic nerve terminals via reversal of reuptake channel. No receptor binding or Ca++ influx 

Term
Methylphenidate
Definition

Indications: ADHD

 

MOA: INDIRECT SYMPATHOMIMETIC - causes release of NE from adrenergic nerve terminals via reversal of reuptake channel. No receptor binding or Ca++ influx

 

Adverse effects: Tachycardia, palpitations, anxiety

 

Contraindications: HTN, atherosclerosis, history of drug abuse, Rx with MAO inhibitors within 2 weeks

Term
Ephedrine
Definition

Indications: pressor agent with anesthesia

 

MOA: INDIRECT SYMPATHOMIMETIC - cause release of NE from adrenergic nerve terminals via reversal of reuptake channel. No receptor binding or Ca++ influx

 

Adverse effects: Tachycardia, palpitations, anxiety

 

Contraindications: HTN, atherosclerosis, history of drug abuse, Rx with MAO inhibitors within 2 weeks

Term
Pseudo-ephedrine
Definition

Indications: nasal decongestion

 

MOA: INDIRECT SYMPATHOMIMETIC - cause release of NE from adrenergic nerve terminals via reversal of reuptake channel. No receptor binding or Ca++ influx

 

Adverse effects: Tachycardia, palpitations, anxiety

 

Contraindications: HTN, atherosclerosis, history of drug abuse, Rx with MAO inhibitors within 2 weeks

Term
Propanolol
Definition

Indications: HTN, angina due to atherosclerosis, MI

 

MOA: non-selective B-blocker; decrease in HR and contractility (B1), increased peripheral resistance due to unopposed a1 receptors, decreased renin release, bronchoconstriction, inhibits effects of epinephrine

 

Adverse effects: bronchospasm, masks symptoms of hypoglycemia, CNS effects including insomnia and depression, some can raise triglycerides, bradycardia

 

Contraindications: DO NOT GIVE B-BLOCKERS TO ASTHMATICS OR PTS WITH COPD, sinus bradycardia, 2nd and 3rd degree heart block, cardiogenic shock **ALSO USE WITH CAUTION IN DIABETICS -- B blockers mask anxiety caused from epi release when pts have low blood sugar

Term
Timolol
Definition

Indications: Glaucoma


MOA: non-selective B-blocker

 

Adverse effects: bronchospasm, masks symptoms of hypoglycemia, CNS effects including insomnia and depression, some can raise triglycerides, bradycardia

 

Contraindications: DO NOT GIVE B-BLOCKERS TO ASTHMATICS OR PTS WITH COPD, sinus bradycardia, 2nd and 3rd degree heart block, cardiogenic shock

**ALSO USE WITH CAUTION IN DIABETICS -- B blockers mask anxiety caused from epi release when pts have low blood sugar

Term
Nadolol
Definition

Indications: long-term angina, HTN

 

MOA: non-selective B-blocker

 

Adverse effects: bronchospasm, masks symptoms of hypoglycemia, CNS effects including insomnia and depression, some can raise triglycerides, bradycardia

 

Contraindications: DO NOT GIVE B-BLOCKERS TO ASTHMATICS OR PTS WITH COPD, sinus bradycardia, 2nd and 3rd degree heart block, cardiogenic shock

**ALSO USE WITH CAUTION IN DIABETICS -- B blockers mask anxiety caused from epi release when pts have low blood sugar

 

Other: has a longer half life (24 hours) than other non-selective B-blockers (4 hours)

Term
Atenolol
Definition

Indications: HTN, angina, MI

 

MOA: B1-antagonist -- reduced heart rate and contractility, decreased renin release, less bronchocontriction in asthmatics than non-selective B-blockers

 

Adverse effects: (typically mild and transient)- depression, insomnia, hypotension, bradycardia

 

Contraindications: sinus bradycardia, 2nd or 3rd degree heart block, cardiogenic shock

Term
Metoprolol
Definition

Indications: HTN, long-term angina

 

MOA: B1-antagonist -- reduced heart rate and contractility, decreased renin release, less bronchocontriction in asthmatics than non-selective B-blockers

 

Adverse effects: (typically mild and transient)- depression, insomnia, hypotension, bradycardia

 

Contraindications: sinus bradycardia, 2nd or 3rd degree heart block, cardiogenic shock

Term
Esmolol
Definition

Indications: Supraventricular tachycardia

 

MOA: B1-antagonist -- reduced heart rate and contractility, decreased renin release, less bronchocontriction in asthmatics than non-selective B-blockers

 

Adverse effects: (typically mild and transient)- depression, insomnia, hypotension, bradycardia

 

Contraindications: sinus bradycardia, 2nd or 3rd degree heart block, cardiogenic shock

 

Other: Esmolol has a very short half-life (~9 min) so it is given i.v. in hypertensive crisis, unstable angina or arrhythmias when longer acting beta blockers may be problematic

Term
Pindolol
Definition

Indications: HTN - especially when sympathetic activity is high

 

MOA: B-antagonist (with partial agonist activity), decreases HR and contractility but bradycardic response is limited, decreases renin release, decreases sympathetic activation

 

Adverse effects: (typically mild and transient)- depression, insomnia, hypotension, bradycardia

 

Contraindications: sinus bradycardia, 2nd or 3rd degree heart block, cardiogenic shock

*USED WHEN PTS ARE LESS TOLERANT OF BRADYCARDIC EFFECTS

Term
Phenoxybenzamine
Definition

Indications: Pheochromocytoma and its related HTN

 

MOA: IRREVERSIBLE non-selective a-blocker, can help to overcome huge outputs of catecholamines from a tumor; inhibits vasoconstriction, increases inotropy and chronotropy due to blockade of pre-synaptic a2 receptor and increased release of NE. Reflex release of NE also occurs in response to hypotension.

 

Adverse effects: prolonged hypotension, reflex tachycardia, nasal congestion

 

Contraindications: coronary artery disease

Term
Phentolamine
Definition

Indications: Test for pheochromocytoma, rx for pheo. before surgery, catecholamine extravasation

 

MOA: reversible non-selective a-blocker

 

Adverse effects: reflex hypotension, reflex tachycardia, nasal congestion

 

Contraindications: coronary artery disease

Term
Prazosin
Definition

Indications: HTN

 

MOA: selective a1-antagonist, inhibits vasoconstriction, less cardiac stimulation than non-selective a-blockers due to preservation of a2-adrenergic function

 

Adverse effects: orthostatic hypotension, syncope

Term
Doxazosin
Definition

Indications: Prostatic hyperplasia, HTN

 

MOA: selective a1-antagonist, inhibits vasoconstriction, less cardiac stimulation than non-selective a-blockers due to preservation of a2-adrenergic function

 

Adverse effects: orthostatic hypotension, syncope

Term
Terazosin
Definition

Indications: Prostatic hyperplasia, HTN

 

MOA: selective a1-antagonist, inhibits vasoconstriction, less cardiac stimulation than non-selective a-blockers due to preservation of a2-adrenergic function

 

Adverse effects: orthostatic hypotension, syncope

Term
Nicotine
Definition

Indications: Withdrawal symptoms of smoking cessation


MOA: Activation of neuronal Nicotinic receptors in autonomic ganglia and CNS


Adverse effects: Irritation at site of administration and dyspepsia

 

 

Term
Succinylcholine
Definition

Indications: Neuromuscular block for electroconvulsive shock therapy or emergency intubation because it has more rapid onset than the non-polarizing drugs


MOA: Depolarizing block of muscle nicotinic receptors;

Phase I - irreversible -- opening of the ion channel depolarizes the motor end plate. Cholinesterase inhibitors augment blockade in this phase. Phase II - after the membrane becomes repolarized, the drug can be overcome with cholinesterase inhibitors or tetanic stimulation. 


Adverse effects: muscle pain from fasciculations, hyperkalemia (from K+ release at Motor End Plate), autonomic problems due to N-ganglion stimulation, cardiac arrhythmia, can initiate malignant hyperthermia in children with undiagnosed muscle myopathies

 

Contraindications: familial hyperthermia, patients with skeletal muscle myopathies, or several days after multiple and wide spread skeletal muscle injury

Term
Acetylcholine
Definition

Indications: None (it is rapidly hydrolyzed by acetyl- AND plasma cholinesterases)


MOA: Nicotinic and muscarinic agonist

 

Term
Methacholine
Definition

Indications: Diagnosis of subclinical asthma, or test for severity of asthma


MOA: Mainly Muscarinic agonist of smooth muscle, glands and the heart


Adverse effects: bronchiolar constriction


Contraindications: Beta-blockers because the antidote to overdose is B-blockers


Notes: longer duration of action than Ach because an additional methyl group slows hydrolysis by acetylcholinesterase; Quaternary Nitrogen Analog

Term
Carbachol
Definition

Indications: Applied to the Conjunctiva as a miotic agent in ocular surgery; to reduce pressure following Cataract surgery


MOA: Muscarinic AND nicotinic receptor agonist; Cannot be hydrolyzed by AchE


Adverse effects: excessive muscarinic and nicotinic receptor activation

 

Notes: Quaternary Nitrogen Analog

Term
Bethanechol
Definition

Indications: Bladder atony; urinary retention


MOA: Muscarinic agonist in GI tract and bladder; resistant to hydrolysis by Both acetyl- and plasma-cholinesterases


Adverse effects: few (because it has less activity on M2 receptors that affect the heart)


Contraindications: peptic ulcer, asthma, bradycardia

 

Notes: Quaternary Nitrogen Analog

Term
Pilocarpine
Definition

Indications: Dry mouth from head and neck radiation or Sjogren's Syndrome; Narrow angle and open glaucoma


MOA: Pure muscarinic agonist, Passes BBB and has CNS effects


Adverse effects: excessive muscarinic toxicity-- slows AV conduction, bronchoconstriction


Contraindications: Beta-blockers

 

Notes: Naturally Occuring Tertiary Amine

Term
Neostigmine
Definition

Indications: Myasthenia gravis; reverses non-depolarizing neuromuscular block


MOA: reversible AchE inhibitor (long effect -- can block Ach from binding AchE for over an hour); direct stimulatory effect on nicotinic receptors at the skeletal muscle endplate (Nm receptors)


Adverse effects: excessive Ach action at peripheral muscarinic and nicotinic receptors


Contraindications: intestinal obstruction

Term
Edrophonium
Definition

Indications: Diagnosis of myasthenia gravis; reversal of neuromuscular block; differential diagnosis between progression of myasthenic weakness and a cholinergic crisis (If you inc Ach more in a pt whose disease is progressing, you should improve their symptoms. On the contrary, if you increase Ach more in a pt who has too much Ach (why they are having muscle weakness) you will exacerbate muscle weakness.)

 

 

MOA: reversible AchE inhibitor; stimulates nicotinic receptors at the NM jxn


Adverse effects: bradycardia, cardiac standstill


Contraindications: mechanical block of intestine and urinary tract

Term
Physostigmine
Definition

Indications: Antidote for muscarinic antagonist poisoning; delerium from anticholinergic drugs; topical treatment for glaucoma


MOA: reversible AchE inhibitor; Passes BBB


Adverse effects: increased Ach at muscarinic or nicotinic receptors - convulsions, respiratory and CV depression


Contraindications: asthma, cardiac insufficiency, intestinal obstruction

Term
Donepezil
Definition

Indications: Alzheimer's Dx

 

MOA: reversible AchE inhibitor; crosses BBB

Term
Pralidoxime (2-PAM)
Definition

Indications: Respiratory muscle weakness in organophosphate poisoning


MOA: Peripheral AchE reactivator -- 

Pralidoxime attaches to the site where a cholinesterase inhibitor (organophosphate) has attached, then attaches to the inhibitor, removing the organophosphate from cholinesterase, allowing it to work normally again. This is known as "regenerating" or "reactivating" acetylcholinesterase allowing the breakdown of Ach at the synapse. 


Notes: Ineffective on "aged" enzyme

Term
Echothiophate
Definition

Indications: Open angle glaucoma


MOA: IRREVERSIBLE AchE INHIBITOR; it is an organophosphate used clinically to produce long term miosis; lasts a long time -- its effect "echoes"


Adverse effects: blurred vision (given in the Elderly, brow ache (typically both resolve)

 

Term
Atropine
Definition

Indications: allay freq. and urge assoc. with cystitis; hypertonic/hypermobile gut; organophosphate (cholinesterase inhibitor) poisoning; bradycardia of vagal origin; induce mydriasis and cycloplegia


MOA: Competitive Muscarinic Antagonist


Adverse effects: "blind as a bat, mad as a hatter, red as a beet, hot as a hare, dry as a bone, the bowel and bladder lose their tone, and the heart runs alone"

 

heart runs alone = tachycardia with respiratory depressions; dry mouth, difficulty swallowing, thirst, hot dry flushed skin, mydriasis, blurred vision and photophobia, tachycardia, inc BP, micturition difficulty, respiratory collapse, nervousness, confusion, hallucinations, muscular incoordination and weakness, inappropriate laughter, psychosis, 

Term
Scopolamine
Definition

Indications: Motion sickness, chemotherapy-induced nausea; anti-salilagogue in surgery; given as a patch


MOA: Competitive Muscarinic Antagonist

 

Contraindications: narrow angle glaucoma

Term
Glycopyrrolate
Definition

Indications: Calms the Gut; anti-salilagogue protects against excessive muscarinic activation during reversal of neuromuscular blockade (given with Neostigmine)


MOA: Muscarinic antagonist


Adverse effects: heat stroke because pt cannot sweat

 

Term
Pancuronium
Definition

Indications: Adjuvant in surgical anesthsia, sp. abdominal wall relaxation and orthopedic procedures


MOA: Non-depolarizing blockade of muscle Nicotinic receptors -- competitive antagonist -- can be overcome by excess Ach (given in the form of AchE inhibitor) or tetanic stimulation; duration of action is shorter than plasma half-life; longest acting of the curare drugs - renal elimination


Adverse effects: Non-analgesic, apnea, muscarinic blockade

 

Contraindications: inhalation anesthetics (enhances effect)

 

Primarily renal excretion

Term
D-tubocurarine
Definition

Indications: Prototype only used in lethal injections


MOA: Non-depolarizing blockade of muscle nicotinic receptors -- competitive antagonist

 

Term
Rocuronium
Definition

Indications: Intubation, muscle relaxation during surgery or ventilation


MOA: Non-depolarizing blockade of muscle Nicotinic receptors -- competitive antagonist -- can be overcome by excess Ach (given in the form of AchE inhibitor) or tetanic stimulation; duration of action is shorter than plasma half-life; eliminated by the liver


Adverse effects: Non-analgesic, apnea, muscarinic blockade

 

Contraindications: inhalation anesthetics (enhances effect)

 

Term
Mivacuronium
Definition

Indications: Intubation, muscle relaxation during surgery or ventilation in pts with renal failure


MOA: Non-depolarizing blockade of muscle Nicotinic receptors -- competitive antagonist -- can be overcome by excess Ach (given in the form of AchE inhibitor) or tetanic stimulation; duration of action is shorter than plasma half-life; shorting acting of the curare drugs --- metabolized by plasma cholinesterase


Adverse effects: Non-analgesic, apnea, histamine release

 

Contraindications: inhalation anesthetics (enhances effect)

Term
Vecuronium
Definition

Indications: Adjuvant in surgical anesthesia, sp. abdominal wall relaxation and orthopedic procedures


MOA: Non-depolarizing blockade of muscle Nicotinic receptors -- competitive antagonist -- can be overcome by excess Ach (given in the form of AchE inhibitor) or tetanic stimulation; duration of action is shorter than plasma half-life


Adverse effects: Non-analgesic, apnea, muscarinic blockade

 

Contraindications: inhalation anesthetics (enhances effect)

Term
Baclofen
Definition

Indications: Spasmolytic drug -- Muscle spasticity associated with Multiple Sclerosis or spinal cord injury


MOA: Inhibits neurotransmitter release from skeletal muscle sensory afferent; GABAB agonist = decreases calcium = reduces the release of excitatory transmitters and substance P in the spinal cord


Adverse effects: Drowsiness, mental disturbances (these side effects can be reduced if given intrathecally)

 

Note: Baclofen can be given orally or through an intrathecal catheter to reduce side effects

Term
Benzodiazepines (eg. Diazepam, Clonazepam)
Definition

Indications: Spasmolytic drug -- Muscle spasm due to local injury (inflammation), muscle spasticity due to loss of descending inhibitory input (eg. cerebral palsy)


MOA: Facilitate GABAA mediated pre-synaptic inhibition; increases Cl- in the cell which hyperpolarizes, inhibiting AP signal for release


Adverse effects: sedation and drowsiness 

 

Contraindications: glaucoma

 

Diazepam = Valium

Term
Tizanidine
Definition

Indications: Spasmolytic drug -- Muscle spasticity due to spinal cord injury or Multiple Sclerosis


MOA: Centrally acting a2-agonist - think "two"zanidine


Adverse effects: Drowsiness, hypotension

Term
Dantrolene
Definition

Indications: Spasmolytic drug -- Muscle spasticity (due to stroke, spinal injury, multiple sclerosis, cerebral palsy); also treats Malignant Hyperthermia (characterized by sudden and prolonged calcium release)


MOA: Blocks calcium release from SR in muscle, thus interfering with E-C coupling; fast muscle fibers are more sensitive, cardiac and smooth muscle insensitive


Adverse effects: muscle weakness, sedation, hepatitis (rare)

 

Term
Morphine
Definition

Indications: Strong analgesia; pain in MI, kidney stones, severe chronic pain, sickle cell (when you get a sickle cell crisis certain muscle areas get ischemic)


MOA: Strong mu opioid receptor agonist


Adverse effects: CAT = Constipation (mu-rec), Addiction, Tolerance; overdose causes asphyxia and death without getting Naloxone immediately


Contraindications:  Triprolidine (CNS depressant), Trovafloxacin (Abx), Rifampin, alcohol

Term
Meperidine
Definition

Indications: Strong analgesic; antispasmotic, biliary spasm, renal colic


MOA: binds K-receptor, K+ channels, muscarinic receptor, dopamine transp. 


Adverse effects: Serotonin Syndrome, seizure, dysphoria, tremor, respiratory distress


Contraindications:  

 

CANNOT be countered with opioid receptor antagonist Naloxone - probably due to its anticholinergic activity

Term
Methadone
Definition

Indications: Strong analgesic; treatment of opioid dependence; cough assoc with terminal lung cancer


MOA: binds mu opioid receptor primarily but also delta opioid receptors and NMDA (glutamate receptor). Firm occupancy of opioid receptors by Methadone (sits in the receptor site for a long time); decreases desire for other opioid intake because it is producing a decrease in effect that stops withdrawal manifestations. With time, addicts can reduce craving.


Adverse effects: prolonged use may result in dependence


Contraindications:  

Term
Hydrocodone
Definition

Indications: Moderately strong analgesic; moderate to severe pain; dry hacking/coughing assoc. with bronchitis; used in surgery to supress coughing


MOA: mu and delta receptor agonist


Adverse effects: addiction due to euphoria and mental numbness

 

Hydrocodone = Vicodin

Term
Codeine
Definition

Indications: Moderately strong analgesic; cough, diarrhea, IBS, narcolepsy


MOA: ?? not fully known. structurally similar to morphine


Adverse effects: physical dependence, urinary retention, depression, constipation, itching, erectile dysfunction

 

Term
Pentazocine
Definition

Indications: Analgesic to relieve mild to moderate pain; dental extraction


MOA: Agonist-antagonists -- act as an agonist at delta and kappa receptors and an antagonist at mu receptors


Adverse effects: Pentazocine weakly antagonizes the analgesic effects of morphine and meperidine; hallucinations, psychomimetic effects, CV effects; some necrosis or sepsis at the injection site


Contraindications:  

Term
Buprenorphine
Definition

Indications: Mild to moderate anesthesia


MOA: Opioid partial agonist

 

Term
Naloxone
Definition

Indications: prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension in overdose; Depersonalization Disorder (DPD)


MOA: opioid receptor antagonist for kappa and delta receptors; high affinity for the mu-opioid receptor in the CNS 


Adverse effects: change in mood, trembling, change in heart rhythm

 

Term
Busipirone
Definition

Indications: Generalized Anxiety Disorder, Depression (off label use with SSRIs)


MOA: 5-HT1A Partial agonist -- activates both pre-synaptic AND post-synaptic receptors which will become desensitized in a couple of weeks and normal amts of serotonin can be released


Adverse Effects: can increase anxiety during initial treatment, drowsiness, nausea


Contraindications: 

Term
Sumatriptan
Definition

Indications: Prophylactic for Migraine


MOA: 5-HT1D Agonist -- inhibition of inflammatory mediator release, cerebrovasoconstriction


Adverse Effects: Coronary vasoconstriction via 5-HT1D receptor


Contraindications: Pts with coronary artery disease

Term
Trazadone
Definition

Indications: Anxiety, Depression (in combination with SSRI)


MOA: Serotonin antagonist-reuptake inhibitor (SARI) that acts on 5-HT2A/2C receptor; SSRI hypnotic, blocks side effects of SSRIs involved in insomnia and sexual dysfunction


Adverse Effects: warning of suicidality in young adults at initiation of treatment


Contraindications: MAO inhibitors

Term
Risperidone
Definition

Indications: Schizophrenia with psychosis (a "positive" symptom as a result of overactivation of dopamine)


MOA: 5-HT2A/D2/3 Antagonist, suppresses DA release in mesolimbic pathway, but increases DA release in mesocortical pathway


Adverse Effects: weight gain, anxiety, akithesia (compulsive need to move), psychosis with abrupt discontinuation

Term
Ondansetron
Definition

Indications: Chemotherapy-induced emesis


MOA: 5-HT3 Antagonist; 5-HT3 is the receptor that is expressed on vago-sensory neurons that stimulate nausea and vomiting in the area-postrema (outside BBB in the brain)


Adverse Effects: not many

Term
Mosapride
Definition

Indications: gastroparesis (delayed gastric emptying)


MOA: 5-HT4 agonist - stimulates Ach release in myenteric plexus


Adverse Effects: Arrhythmia (long QT Syndrome)

 

Term
Fluoxetine
Definition

Indications: Depression, OCD, PTSD, panic disorder, social phobia


MOA: SSRI; 5-HT transporter (reuptake) inhibitor


Adverse Effects: Sexual dysfuncion, insomnia


Contraindications: MAO inhibitor

 

Fluoxetine = Prozac

Term
Sertraline
Definition

Indications: Depression, OCD, PTSD, panic disorder, social phobia


MOA: SSRI; 5-HT transporter (reuptake) inhibitor


Adverse Effects: Sexual dysfuncion, insomnia


Contraindications: MAO inhibitor

 

Sertraline = Zoloft

Term
L-DOPA
Definition

Indications: Parkinson's Disease


MOA: D1/2 Agonist; increases DA release in nigrostriatal pathway


Adverse Effects: Arrhythmia, nausea, anxiety, hallucinations, dyskinesia and motor fluctuations

Term
Carbidopa
Definition

Indications: Parkinson's Disease; concurrent with L-DOPA to reduce peripheral DA production 


MOA: inhibits AADC in peripheral tissue - AADC converts L-DOPA to dopamine but dopamine cannot cross BBB

 

Adverse Effects: augments SE of L-DOPA in CNS

Term
Bromocriptine
Definition

Indications: Parkinson's Disease


MOA: ergot alkaloid with D2 agonist properties; post synaptic activation in basal ganglia, may also be neuroprotective (antioxidant, free radical scavenger, reduction of DA turnover) therefore, best used early in disease course

 

Adverse Effects: cardiac valvular fibrosis (long term use); impulse control disorders (relatively rare)

Term
Selegiline
Definition

Indications: Parkinson's Disease (lower doses); Depression (higher doses)


MOA: Selective inhibition of MAO-B which metabolizes dopamin; can block MAO-A* at high doses

 

Adverse Effects: hypotension, dry mouth; at higher doses can cause hypertensive crisis or serotonin syndrome

 

Contraindications: concomitant use of indirect acting sympathomimetics or drugs that increase serotonin neurotransmission

 

MAO-A degrades tyramine in the digestive tract

Term
Tolcapone
Definition

Indications: Parkinson's Disease (more advanced)


MOA: inhibits COMT; prolongs and increases effect of L-DOPA, reduces "off" time, can reduce amount of L-DOPA dosing required

 

Adverse Effects: dyskinesia, hallucinations, nausea, hypotension

 

Contraindications: liver failure

Term
Haloperidol
Definition

Indications: Acute psychosis, long-term depot for poorly compliant schizophrenic patients


MOA: D2 antagonism

 

Adverse Effects: extrapyramidal motor disturbances

Term
Methylphenidate
Definition

Indications: ADHD


MOA: DA reuptake inhibitor; increased DA release in frontal cortex

 

Adverse Effects: tachycardia

 

Contraindications: TCA, arrhythmia, HTN

Term
Metaclopramide
Definition

Indications: Chemotherapy-induced and post-OP nausea and vomiting; gastroparesis


MOA: D2 antagonist (blocks nausea in Emetic Center and Area Postrema), also has 5-HT4 agonist properties

 

Adverse Effects: akathisia, focal dystonia

 

Contraindications: long-term rx (3 months can cause tardive dyskinesia)

Term
Procaine
Definition

Indications: local anesthetic, nerve block, subarachnoid


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; potency = 1, metabolized by plasma cholinesterase -- short duration (30-45 min); often combined with epinephrine


Adverse Effects: PABA-induced allergy

 

Ester Local Anesthetic

Term
Cocaine
Definition

Indications: topical local anesthetic


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; potency = 2, metabolized to PABA by plasma cholinesterase; useful becuase it is the only LA that vasoconstricts; prevents reuptake of NE at adrenergic terminals


Adverse Effects: HTN, tachycardia, dependence, PABA allergy, CNS toxicity

 

Contraindications: HTN, alpha-agonist

 

Ester Local Anesthetic

Term
Tetracaine
Definition

Indications: spinal anesthesia (subarachnoid anesthetic)


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; potency = 16 because it is more lipophilic, metabolized to PABA by plasma cholinesterase; long lasting (2-5 hours) 

 

 

Ester Local Anesthetic

Term
Benzocaine
Definition

Indications: topical local anesthetic


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; it is a PABA ester that is poorly water soluble and can be applied as dusting powder or ointment to wounds or ulcerated surfaces without concern for systemic toxicity

 

 

Term
Lidocaine
Definition

Indications: epidural/subarachnoid, infiltration, nerve block, 


MOA:  
bind and blocks open or inactivated channels on the cytoplasmic side; epinephrine is effective for inducing vasoconstriction; high hepatic extraction; not highly protein bound in the plasma

 

Adverse Effects: CNS toxicity before CV toxicity, Transient Neurologic Symptoms (TNS)

 

Contraindications: arrhythmias, hypotension

 

amide

Term
Mepivacaine
Definition

Indications: infiltration, nerve block, epidural


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; epinephrine is effective for inducing vasoconstriction

 

Adverse Effects: seizures, CV toxicity, early transient neurobehavioral effects in neonates

 

amide

Term
Bupivacaine
Definition

Indications: infiltration, nerve block, epidural - permits motor activity of abdominal muscles (B = Baby), subarachnoid; postoperative analgesia


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; epinepherine not effective because it is highly protein bound; particularly prolonged duration of action (24 hours); more potent and more toxic than mepivacaine and lidocaine

 

Adverse Effects: CNS toxicity, more cardiotoxic than others [Although all local anesthetics potentially shorten the myocardial refractory period, bupivacaine avidly blocks the cardiac sodium channels, thereby making it most likely to precipitate malignant arrhythmias --- treat toxicity with INTRALIPID] 

 

amide

Term
Ropivacaine
Definition

Indications: epidural


MOA:  bind and blocks open or inactivated channels on the cytoplasmic side; epinepherine not effect because it is highly protein bound

 

Adverse Effects: CNS activation, seizures, less cardiotoxic than bupivacaine, produces less of a motor block


Contraindications: Bowel obstruction because of increased motility

 

amide

Term
Nitrous Oxide (N2O)
Definition

Indications: Gaseous anesthesia used in conjugation with other drugs in anesthesia


MOA:  NOT blood soluble, fast induction, okay for asthmatics (bronchodilator)

 

Adverse Effects: respiratory depressant (like all inhaled anesthetics, but metabolic O2 consumption decreases too)

Term
Halothane
Definition

Indications: Volatile anesthesic 


MOA:  very blood soluble, slow induction, HR stays the same (other VAs inc), baroreceptor reflex decreases (other VAs stay the same), CO decreases (other VAs stay the same or inc) 

 

Adverse Effects: almost never used today because of its sensitization to catecholamines and its potential to cause liver necrosis

Term
Isoflurane
Definition

Indications: Volatile anesthesic 


MOA:  less blood soluble and faster induction than Halothane; maintains CO; advantage of not raising the intracranial pressure in neurosurgery

 

Adverse Effects: 

Term
Sevoflurane
Definition

Indications: Volatile anesthesic 


MOA:  less blood soluble and faster induction than Isoflurane; maintains CO; advantage of being pleasant-smelling and non-irritating to the airway; rapid induction and recovery making it especially suitable for brief outpatient procedures; minimal cardiac effects making it suitable for elderly

 

Adverse Effects: degraded by CO2 to Compound A which is potentially nephrotoxic

Term
Desflurane
Definition

Indications: Volatile anesthesic 


MOA:  lowest blood solubity and fastest induction of the fluranes

 

Adverse Effects: "des" advantages = irritating to airway, increased HR, BP (due to sympathetic activation) and intracranial edema

Term
Thiopental
Definition

Indications: Ultrashort-acting barbiturate; General IV anesthetic; used for rapid induction of unconsciousness


MOA:  rapid entry into the CNS is followed by a relatively quick redistribution to indifferent tissues because it is lipid soluble; "Robinhood Phenomenon"; fast recovery; useful in neurosurgical procedures because it markedly reduces intracranial pressure; stimulates inhibitory neurons = increases GABA

 

Adverse Effects: poor analgesic because it can increase the sensitivity to pain when administered in inadequate amounts; arterial contraction (due to baroreceptors reflex), venous hypotension, decreases respiration

Term
Methohexital
Definition

Indications: Ultrashort-acting barbiturate; induces general anesthesia; anesthetic before electroconvulsive therapy for depression; epileptic cerebral mapping


MOA:  rapid entry into the CNS is followed by a relatively quick redistribution to indifferent tissues because it is lipid soluble; shows some excitatory phenomena on EEG

 

Adverse effects: reduces seizure threshold 

 

Thiopental is preferrable to use to induce anesthesia in epileptics. 

 

Term
Ketamine
Definition

Indications: General IV Anesthetic


MOA:  NMDA antagonist (NMDA is a glutamate receptor); has more of a CENTRAL mechanism of action, depresses cortical function, stimulates limbic system including hippocampus; pts may appear awake; strong feeling of dissociation from the environment; can be administered i.m. - good for kids

 

Adverse Effects:  excitatory or hallucinatory phenomena as pt emerges from anesthesia; increased ICP, increased cerebral oxygen needs

 

Contraindications: psychiatric disorders, HTN, high ICP or head trauma

Term
Etomidate
Definition

Indications: General IV Anesthetic used only for induction


MOA:  enhances GABA-ergic actions; potent hypnotic agent; good for VERY SICK pts such as those with CV disease, inc ICP, trauma, aneurysm; no hypotensive effects


Adverse Effects:
  pain on injection, myoclonus, could suppress adrenocortical fxn 

 

Contraindications: Epileptic pts (shows stimulation on EEG), Addison's Dx (Chronic Adrenal Insufficiency)

Term

Propofol

Definition

Indications: General IV Anesthetic (prepared in a fat solution - need to use antimicrobial with it)


MOA:  rapid -- peak effect in 60 seconds; currently favored in surgery (sense of well-being on emergence); enhances GABA-ergic actions; similar to barbiturates except it inhibits the baroreflex and induces peripheral arterial vasodilation


Adverse Effects:
 myoclonus, pain on injection, apnea during induction, hypotension

 

Contraindications: kids (could cause metabolic acidosis), asthmatics 

 

*killed Michael Jackson

Term
Fentanyl
Definition

Indications: Opioid mu agonist; strong analgesic used as a supplement in surgery


MOA:  80 times more potent than Morphine; does not cause histamine release like morphine so larger doses are tolerated without CV effects; given transdermally


Adverse Effects:
  respiratory depressant, delay in wakening

 

 
Term
Aspirin
Definition

Indications: 

low dose: (anti-platelet activity = permanently inhibits COX-1 through acetylation which prevents the platelets from making TXA-2) prevention of stroke and MI in pts with high rist of CVD; treatment in acute occlusive stroke; prevention of CVD after MI, stroke, angina, bypass

high dose: (anti-platelet effect of inhibiting TXA2 is offset by increasing inhibition of endothelium-derived PGI2) analgesic, anti-pyretic, anti-inflammatory


MOA:  Non-selective inhibitor of BOTH COX-1 and COX-2; UNIQUE mechanism compared to other NSAIDs -- irreversibly inhibits COX-1 by acetylating the enzyme within its active site thereby inhibiting the binding of the arachidonic substrate; also acetylates COX-2 although it is a much less potent inhibitor of this enzyme

 *can be ZERO-ORDER kinetics at high doses

 

Adverse Effects: delayed onset of labor, early closing of ductus arterious in fetus; salicylate intoxication = hyperthermia, hyperventilation, metabolic acidosis, hypoglycemia, confusion, tremors, seizure, coma and death

 
Contraindications: gout pts (decreases uric acid elimination), GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, elderly, children with febrile viral infections (risk of Reye's Syndrome); All salicylates are 50-90% protein bound- high potential for drug interactions e.g. warfarin, sulfonylureas
Term
Ibuprofen
Definition

Indications: Traditional NSAID -- inflammation, pain, fever

Rapid onset of action, ideal for fever and acute pain


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD
Term
Naproxen
Definition

Indications: Traditional NSAID -- inflammation, pain, fever

rapid onset of action  (IDEAL FOR ANTI-PYRETIC), long serum half-life of 14hours = twice-daily dosing


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: considered to be one of the safest NSAIDs; GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD, children with febrile viral infections, gout
Term
Oxaprozin
Definition

Indications: Traditional NSAID -- inflammation, pain, fever; long serum half-life of 50-60 hours = once daily dosing; used in treatment of gout (increases excretion of uric acid)


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD, children with febrile viral infections, gout
Term
Indomethacin
Definition

Indications: Traditional NSAID -- analgesis, potent anti-inflammatory, anti-pyretic; used to close patent ductus arteriosus 


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: greater toxicity than the other tNSAIDs; GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD, children with febrile viral infections, gout
Term
Diclofenac
Definition

Indications: Traditional NSAID -- potent analgesic, anti-inflammatory, anti-pyretic; relatively selective for COX-2


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: increased risk of MI or stroke; GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD, children with febrile viral infections, gout
Term
Keterolac
Definition

Indications: Traditional NSAID -- mainly used as an IV analgesic for moderate/severe post-surgical pain; used as a replacement for opioid analgesics (eg. morphine)


MOA:  inhibition of COX activity by preventing the production of prostaglandins

 

Adverse Effects: GI and stomach (inhibition of COX-1 that acts to inc PG --> mucous), Renal, CV system, liver, anti-platelet, hypersensitivity, CNS, skin, photosensitivity, pregnancy - D.A. does not close

 
Contraindications: GI ulcers, bleeding disorders or on anti-coagulants, hypersensitivity to any NSAIDs, pregnant, renal disorders, risk of CVD, children with febrile viral infections, gout
Term
Celecoxib
Definition

Indications:  NSAID - analgesic, anti-inflammatory, anti-pyretic; preferrable in pts with a prior history of GI bleeds and/or ulcers


MOA: COX-2-specific inhibitor; off-target effect (independent of COX-2 effect) that acts on Na+ ion channels in vascular smooth muscle to promote vasodilation

 

Adverse Effects: heart and kidney risks 

 
Contraindications: pts with CVD risk; renal disease; rheumatoid arthritis
Term
Acetaminophen
Definition

Indications:  mild to moderate pain and fever not associated with inflammation


MOA: metabolized selectively in the brain to an active metabolite (AM404) that inhibits COX-2 in the CNS and acts on the endogenous cannabinoid system in the pain and thermoregulatory centers; does not effectively inhibit either COX-1 or COX-2 expressed in the periphery

 

Adverse Effects: free of adverse effects a normal doses; hepatoxicity at higher doses

 
Contraindications: liver disease
Term
Diflusinal
Definition

Indications: Salicylate -- anti-inflammatory, analgesic


MOA:  inhibits COX-1 and COX-2; does not cross the BBB = ineffective anti-pyretic; lower risk of adverse effects than aspirin because salicylates are non-acetylated and are unable to irreversibly inhibit COX2

 

Adverse Effects: increased risk of GI complications (e.g. gastric ulcers); increased risk of  bleeding (e.g. hemophiliacs); salicylate intoxication = hyperthermia, hyperventilation, metabolic acidosis, hypoglycemia, confusion, tremors, seizure, coma and death

 

Contraindications:  All salicylates are 50-90% protein bound- high potential for drug interactions e.g. warfarin, sulfonylureas


 

 
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