Exam II Drugs Flashcards by Jonathan Miller

What Anticonvulsant blocks Na+ and Ca+ channels, decreases glutamate release, Used in tonic clonic, partial, absence and bipolar affective illness, And has side effects of Dizziness, headache, diplopia, Steven Johnson syndrome, Newer drug, similar to phenytoin with fewer side effects, lower plasma protein binding of 55% compares to phenytoin 75-95%

Lamotrigine

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What anticonvulsant decreases Na+ influx and decreases release of glutamate, is used in partial and tonic clinic seizures, induces cytochrome p450, has saturable elimination, Decreases folic acid: fetal hydantoin syndrome; gingival hyperplasia; hirsuitism; nystagmus, diplopia, ataxia, neuropathy, sedation, megaloblastic anemia, SLE-like syndrome, lymphadenopathy, Steven Johnson syndrome, osteopenia

Phenytoin

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What Anticonvulsant Blocks Na+ and Ca+ channels and antagonizes cholinergic receptors, Used in partial and tonic clonic drug of choice, trigeminal neuralgia; bipolar disorder, Induces cytochrome P450, contraindicated with excess alcohol consumption, and has the side effects of Agranulocytosis, liver toxicity (check LFTs), and aplastic anemia; fetal hydantoin syndrome, diplopia, ataxia, Steven Johnson syndrome

Carbamazepine

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What Anticonvulsant Blocks Na+ and Ca2+ channels, used for partial and tonic clonic, trigeminal neuralgia; bipolar disorder, is a Newer drug, similar to carbamazepine with fewer side effects, lower plasma protein binding of 40% than carbamazepine 75-95%, and has side effects of Agranulocytosis, liver toxicity (check LFTs), and aplastic anemia; fetal hydantoin syndrome, diplopia, ataxia, Steven-Johnson syndrome, induces cytochrome P450

Oxcarbazepine

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What Anticonvulsant blocks Na+ channels, blocks T-type Ca2+ channels, and increases GABA concentration by inhibiting GABA transferase, is used for partial, absence, and tonic clonic; migraine; prophylaxis of cluster headache, relieves mania better than lithium; bipolar disorder, and has the side effects of Liver toxicity, pancreatitis, potentially fatal, teratogen: spina bifida, tremor, weight gain

Valproate (valproic acid)

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What Anticonvulsant blocks T-type Ca2+ channels, is used for Absence seizures “Sux to have absence seizures”, and has the side effects of Nausea, headaches, dizziness, hyperactivity, GI, fatigue, urticaria, Steven Johnson syndrome?

Ethosuximide

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What anticonvulsants inhibit T type calcium channels and can be used for absence seizures?

Ethosuximide and valproate

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What opioid is a Strong mu opioid agonist to modulate synaptic transmission – opens K+ channels, closes Ca2+ channel decreased synaptic transmission, inhibits the release of Ach, NE, 5HT, glutamate, and substance P; chronic oral dose converted to more potent morphine-6-glucoronide, also acts on kappa receptors in dorsal spindle cord, is used for Chronic and severe pain analgesic: strong agonist, general anesthetic, antitussive, antidiarrheal, acute pulmonary edema, anxiety relief, Low oral: parenteral ratio, contraindicated with dialysis because increased M3G in circulation will lead to seizures and has the side effects of Respiratory depression, histamine release, constipation, nausea, miosis, addiction liability, convulsions

Morphine

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What opioid is a Partial moderately strong mu opioid agonist to modulate synaptic transmission – opens K+ channels, closes Ca2+ channels decreased synaptic transmission, inhibits the release of Ach, NE, 5HT, glutamate and substance P, used for Severe pain analgesic: strong agonist, general anesthetic, Medium oral: parenteral ratio, and has the side effects of Respiratory depression, constipation, nausea

Oxycodone

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What opioid is a Strong mu opioid agonist – synthetic, modulate synaptic transmission – opens K+ channels, closes Ca2+channels decreased synaptic transmission, inhibits the release of Ach, NE, 5HT, glutamate and substance P, is used for Maintenance therapy for opioid addiction, withdrawal from opioid dependence, pain analgesic: strong agonist, High oral: parenteral ratio, has the side effects of Respiratory depression, histamine release, constipation, nausea, miosis, addiction liability, convulsions?

Methadone

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What opioid is a weak naturally occurring Partial mu opioid agonist modulate, far lower abuse potential than morphine, synaptic transmission – opens K+ channels, closes Ca2+channels decreased synaptic transmission, inhibits the release of Ach, NE, 5HT, glutamate and substance P, is used for Mild-moderate pain, antitussive, Converted to morphine by CYP2D6 10%, high oral: parenteral ratio, and has the side effects of Respiratory depression, severe constipation, addiction liability, convulsions?

Codeine

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What opioid is a Strong mu opioid agonist is used for Pain, acute migraine attacks, shivering, Contraindicated in patients with MAO-I (results in hyperpyrexia), tachycardia, and has the side effects of CNS excitation at high doses, histamine release, antimuscarinic effects, less severe respiratory depression, constipation, biliary colic, urinary retention?

Meperidine

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What opioid is a Strong mu opioid agonist, is used for Pain analgesic: strong agonist, general anesthetic, adjunct anesthesia (induction)
And has the side effects of Prolonged recovery, nausea, Low oral: parenteral ratio, metabolized by P450?

Fentanyl

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What opioid is a Mixed partial mu agonist and kappa antagonist action, at high doses acts as a mu antagonist, is used in Treatment of opioid/cocaine dependence, pain analgesic: mixed agonist-antagonist, sublingual route preferred to avoid first pass elimination, has the side effects of Respiratory depression, sedation, nausea, vomiting, slow mu receptor dissociation thus antagonizing other opioids

Burepinorphine

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What opioid is Unknown but hypothesized strong or partial mu agonist, used as Antitussive

Dextromethorpan

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What opioid is an Antidiarrheal?

Diphenoxylate

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What opioid is an Antidiarrheal – similar to opioid agonist

Oral antidiarrheal

Loperamide

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What opioid is a Partial mu opioid agonist, Pain analgesic – strong agonist, antitussive, analgesic, mild to moderate pain, Medium oral: parenteral ratio

Hydrocodone

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What is an Antagonist of all opioids, Drug of choice for opioid antagonism, 1-2 hours, Ineffective to use against barbiturate overdose, but safe

Naloxone

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What is an Antagonist of all opioids, Longer action than naloxone 10.5 hours, can be used orally

Naltrexone

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What drug is a Dopamine precursor, is used in PD, and can cause Nausea, orthostatic hypertension, psychosis, compulsive behaviors, dyskinesia, Crosses the BBB, contraindicated with MAO-A inhibitor

Levodopa (L-Dopa)

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What drug Inhibits AAAD in periphery, is used in PD, may cause Nausea, orthostatic hypertension, psychosis, compulsive behaviors, dyskinesia, Does not cross BBB, contraindicated with MAO-A inhibitor

Carbidopa

What drug is a COMT inhibitor, peripheral, is used in PD, and can cause Dyskinesia, nausea, somnolence, orthostatic hypertension

Entacopone

What drug is a COMT inhibitor, peripheral and central, used in PD, and can cause Dyskinesia, nausea, somnolence, orthostatic hypertension

Tolcapone

What drugs are MAO-B Inhibitor, are used in PD, L-dopa adjunct – delays start, Contraindicated with MAO-A inhibitor

Selegiline, rasageline

What drug is a Dopamine receptor agonist, D2 preferred, used in PD, May cause Nausea, orthostatic hypertension, hallucinations, somnolence, dyskinesia?

Ropirinole

What drug is a Dopamine receptor agonist, D3 preferred, used in PD, and may cause Nausea, orthostatic hypertension, hallucinations, somnolence, dyskinesia

Pramipexole

What drug is an Anticholinergic, is used in PD for tremor and has Anti-PS effects?

Benztropine

What drug is an Anti-viral – antiparkinsonian, inhibits fusion of lysosomes; inhibits viral penetration and uncoating; increases release of endogenous dopamine, is used in PD, may cause CNS effects (ataxia, dizziness, slurred speech, nervousness, seizure), anticholinergic, orthostatic hypotension?

Amantadine

What drug is an Anti-migraine – agonist at 5HT-1D/B receptors; these receptors are responsible for vasoconstriction and blockade of CGRP vasoactive neuropeptide release (inhibits neurogenic inflammation, block neurogenic plasma extravasation in dura) in the vessel wall during the activation of the trigeminal-vascular system, decrease NT release, is used for Acute attack of migraine, abortive treatment of cluster headache, and is Contraindicated with coronary vasospasms, so avoid with patients with ischemic heart disease or coronary artery spasm, vasospasms, in combination with other 5HT elevating drugs, or in migraines due to vasoconstriction , serotonin syndrome

Sumatriptan

What drug is an Anti-emetic – serotonin antagonist, 5HT3 blocker (ligand bound), is used for Nausea (caused by cancer therapy or postoperative state) and has the side effects of Headache, constipation, dizziness, Serotonin syndrome?

Ondansetron

What drug is an Anti-migraine – 5HT2 antagonist via partial agonism/antagonism with non-specific effects on 5HT1, DA, and NE receptors, weak vasoconstrictor, ergot derivative related to LSD, is used for Prophylaxis of migraine and cluster headaches, Contraindicated in patients with peripheral vascular disease, coronary artery disease, and pregnancy; patient placed on drug holiday to prevent tachyphylaxis and can cause the side effects of GI distress, inflammatory fibrosis of kidney, endocardium, retroperitoneum, cardiac valve, and pleuropulmonary fields; thickening of cardiac valve; lung, and cardiac valves, nausea, vomiting, diarrhea?

Methylsergide

What drug is a Serotonin 5HT2A/C antagonist, Prevents vasoconstriction and bronchospasm of carcinoid syndrome Hypertension, may cause carcinoid syndrome associated with carcinoid tumor, contraindicated for patients with Hypotension?

Ketanserin

What drug is an Antihistamine – serotonin/H1 antagonist; antipruritic, 5HT3 agonist, Decreases diarrhea in carcinoid tumors; decreases dumping syndrome may cause Weight gain?

Cyproheptadine

What drug is a Serotonin synthesis inhibitor?

p-chlorophenylalanine

What drug is an Antimigraine – partial 5HT2 agonist at some blood vessels, non-selective 5HT antagonist at smooth muscle, causes smooth muscle contraction, vasoconstriction, reversible alpha receptor blockade, is used for Acute cluster and migraine headache treatment; cluster headache prophylaxis, Contraindicated in pregnant patients or patients with cardiovascular disease or coronary artery disease, contraindicated if migraine headache due to vasoconstriction or spasm, Raynaud’s syndrome, severe, uncontrolled hypertension, hyperthyroidism, sepsis, porphyria, hepatic or renal disease and may cause Nausea by direct action on CTZ, leg weakness and muscle pain, numbness in fingers and toes, constricts arteries and veins, gangrene as a result of vasoconstriction

Ergotamine

What drug is a Carbonic anhydrase inhibitor, diuretic, inhibits carbonic anhydrase on PCT and DCT, which prevents HCO3- reabsorption; lose Na+, HCO3-, and K+ in urine, is used for Glaucoma, high altitude, metabolic alkalosis; alkalinization of urine, epilepsy, Weak diuretic because other sites further downstream along the nephron can compensate for sodium loss; causes decreased secretion of HCO3- in aqueous humor and has the side effects of Hyperchloremic metabolic acidosis, sulfa drug allergy, neuropathy, and ammonium toxicity

Acetazolamide

What drug Irreversibly inhibits COX enzyme by covalent acetylation, platelets cannot synthesize new enzyme so the effects last until new platelets are produced, increase bleeding time, decrease TXA2 and prostaglandins, us used for Antipyretic, analgesic, anti-inflammatory, antiplatelet, decreased aggregation, has the side effects of Gastric ulceration, tinnitus, chronic use can lead to acute renal failure interstitial nephritis, and upper GI bleeding, Reye syndrome in children with viral infection, overdose causes respiratory alkalosis initially, which is then superimposed by metabolic acidosis

Aspirin

What drug is a Stimulant – adenosine receptor blocker; stimulates CNS and cardiac muscle; relaxes smooth muscle; produces diuresis; increases cerebrovascular resistance acute migraine attack, used for Acute migraine attack, Crosses placenta into breast milk Avoid in patients with peptic ulcer because it stimulates gastric mucous secretions?

Caffeine

What drug is an Antiarrhythmic (class 1B), anesthetic agent, blocks Na+ channels intracellularly, used as a Local anesthetic; ventricular tachycardia, Given with epinephrine to maintain locality and increase duration of anesthetic properties via epinephrine mediated vasoconstriction, may cause Sleepiness, light-headedness, visual/audio disturbances, restlessness, nystagmus, shivering, tonic-clonic convulsion, death?

Lidocaine

What drug is a Non-dihydropyridine L-type Ca2+ channel blocker – block voltage gated Ca2+ channels of cardiac smooth muscle, is used for Hypertension, angina pectoris, arrhythmia, cluster headaches prophylaxis, Contraindicated with atrioventricular block, hypotension, and bradycardia, may cause Cardiac depression, peripheral edema, flushing, dizziness, and constipation?

Verapamil

What drug is a Ca2+ channel blocker and used in subarachnoid hemorrhage?

Nimodipine

What drug is a Tricyclic antidepressant – inhibit reuptake of NE and 5HT at neuronal synapses, is used for Major depression, panic disorder, sedative, prophylaxis for migraines, Contraindicated with hypotension arrhythmia, conduction deficits, glaucoma and may cause Sedation, alpha blocking effects (orthostatic hypertension), anticholinergic (tachycardia, dry mouth, and urinary retention), hallucinations (in elderly), and confusion (in elderly); overdose toxicity results in convulsions, coma, cardiotoxicity (arrhythmias), respiratory depression, and hyperpyrexia?

Amitriptyline

What drug is an Inhalational anesthetic – dilates coronary arteries and decreases myocardial oxygen consumption, safe in patients with ischemic heart disease; potentiate GABA-A receptors, glycine receptors, and K+ channels receptors; inhibit glutamatergic and nAch receptors, is used as a General anesthetic, Best muscle relaxant, most widely used, 99% excreted unchanged in the lungs, 1.4% MAC,

Isofluorane

What drug is a Weak inhalational anesthetic agent – blocks the NMDA-R like ketamine; gas, strong analgesic agent, is used as a General anesthetic, potent analgesic, anesthetic adjunct (maintenance), 99.9% excreted in the liver, incomplete anesthetic >100%MAC, 0% metabolized in the liver, O2 given to get pt. off it; contraindicated with pneumothorax and obstructed bowel loop and can cause Hypoxia – rapidly diffuses out to alveoli and dilutes oxygen in the lung, nausea, vomiting?

Nitrous oxide

What drug is a IV anesthetic agent – barbidurate, prolongs IPSP duration, is used as an Antiepileptic; cerebral edema; anesthetic (stage 3 anesthetic), used during induction of anesthesia and deep sedation, Depresses CNS in less than 1 min, poor analgesic, may cause Laryngospasm during stage 3 induction, decreases cerebral metabolism and blood flow so ok to use in pts. with cerebral swelling, decreased cardiac output and blood pressure?

Thiopental

Whist drug is a Benzodiazepine; short acting, IV anesthetic agent, is used for Preanesthetic medication; produces antegrade amnesia (loss of memory of events after administration) calming down the patient, anxiolysis, and sedation (premedication) may cause Circulatory and respiratory depression, decreases cardiac output and blood pressure Flumazenil antagonizes CNS depression caused by benzodiazepines, ok to use in patients with cerebral swelling?

Midazolam

What drug is an IV anesthetic agent; blocks NMDA-type glutamate receptors, is used as a General anesthetic, Contraindicated with psychosis, increased infusion does not significantly increase half life, and may cause Dissociative anesthesia, catatonia, hallucinations, amnesia, and analgesia without loss of consciousness, increased heart rate and cardiac output, increased intracranial pressure, postoperative hallucinations

Ketamine

What opioids that are also used in anesthesia are Opioid agonist; IV , afe used for general pain, general anesthetic, induction and maintenance in total intravenous anesthesia, epidural anesthesia with local anesthetics, ICU-conscious and deep sedation, maintenance can be reversed by naloxone and have a prolonged recovery, nausea, chest wall rigidity, impaired ventilation, respiratory depression, decreases heart rate and blood pressure?

Fentanyl, sufentanil, remifentanil (ultra-short)

What drug is an IV anesthetic agent – potentiates GABA-A receptors, is used as a General anesthetic, fast acting for ambulatory or outpatients, induction, maintenance, Not a good analgesic, increased infusion does not significantly increase half life, and may cause Seizure, decreases intracranial pressure, respiratory depression?

Propofol

What drugs arean Anesthetic agent, ester – blocks Na+ intracellularly, is used as a Local anesthetic, Hydrolyzed by plasma esterase and may cause Sleepiness, lightheadedness, visual/audio disturbances, restlessness, nystagmus, shivering, tonic clonic convulsions, death?

Procaine, Tetracaine

What drug is an Antiarrhythmic (class 1B), anesthetic agent, amide – blocks Na+ channels intracellularly, used for Local anesthetic, ventricular tachycardia, Given with epinephrine to maintain locality and increase duration of anesthetic properties via epinephrine mediated vasoconstriction, longer duration, metabolized by the liver, shorter duration, may cause Sleepiness, lightheadedness, visual/audio disturbances, restlessness, nystagmus, shivering, tonic clonic convulsion, death, CNS excitation, cardiovascular collapse

Lidocaine

What drug is a Local anesthetic amide – blocks Na+ channels intracellularly may cause Severe cardiovascular toxicity, Has a Longer duration, metabolized by the liver?

Bipuvacaine