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BIOM3090 Final Drugs
list of cardiovascular, CNS, and anesthetic drugs
56
Pharmacology
Undergraduate 3
04/16/2013

Additional Pharmacology Flashcards

 


 

Cards

Term

Clonidine

Definition
  • hypertension, sedative, opioid withdrawal
  • centrally acting sympatholytic
  • α-2 agonist = ↓ cAMP = inhibitory
  • can also ↓ aqueous humor in the eye to ↓ intraocular pressure
  • causes ↓ ACh release ➞ ↓ M3 activation in GI ➞ ↓ GI motility (constipation or treat diarrhea 
  • α2 agonist in respiratory ➞ ↓ respiration
  • ↓ NE in CNS = ↓ SNS and ↑ PSNS = ↓ CO + PVR
Term

Propanolol


Definition
  • hypertension, heart failure + excessive tachycardia, angina, arrhythmia 
  • non-selective β-blocker
  • ↓ HR and CO
  • b/c ↓ HR ➞ vasoconstriction of organ and skin
  • used frequently
  • also causes: ↓ secretion in eye, contraction of smooth muscle, and vasoconstriction in skeletal muscle
  • toxicities are with β2 blockade (asthma)
Term

Metropolol

Definition
  •  hypertension, heart failure + excessive tachycardia, angina, arrhythmia
  • selective β1-blocker
  • block β1 in heart = ↓ CO
  • b/c ↓ HR body compensates ➞ vasoconstriction
  • block β1 in juxta-glomerular of kidney = ↓ renin release = ↓ PVR
  • also causes: ↓ secretion in eye
Term

Prazosin

Definition
  • hypertension
  • selective α1-blocker
  • block α1 in arterioles and venules = relax blood vessels
  • body compensates with ↑ HR and ↑ renin = may need diuretics or β-blockers too
  • also causes: relaxation of dilator muscle, ↑ secretion in eye, relaxation of sphincters, relaxation of pilomotor muscles
  • toxicity = rare and mild (dizziness and headache)
Term

Sodium Nitroprosside

Definition
  • hypertension
  • nitric oxide donor
  • used in emergencies (short-acting)
  • toxicities = hypotension and cyanide accumulation
Term

 Varapamil

Definition
  • hypertension, angina, arrhythmia
  • calcium channel blocker 
  • inhibits calcium influx into atrial smooth muscle cells ➞ relaxation ➞ vasodilation
  • toxicity = bradycardia
Term

Enalapril

Definition
  •  hypertension, mild heart failure, left ventricular dysfunction (no edema)
  • ACE inhibitor
Term

Losartan

Definition
  • hypertension, mild heart failure, left ventricular dysfunction (no edema)
  • AT1 receptor blocker
  • effectiveness similar to ACE inhibitor
Term

Hydrochlorotriazide

Definition
  • hypertension, mild heart failure, heart failure + edma
  • thiazide diuretic
  • inhibit NaCl transport in distal convoluted tubule = ↑ NaCl in urine = ↑ H2O in urine = ↓ blood volume = ↓ BP
  • toxicities: hypokalemia, gout, dehydration
Term

 Furosemide

 

Definition
  • hypertension
  • loop diuretic
  • inhibits cotransport of Na+, K+, and Cl- = inhibit NaCl reabsorption inhibited 
  • severe hypertensino and pulmonary edema
  • toxicities: same as hydrochlorotriazide, and does-dependent ototoxicity (hearing loss)
Term

Digoxin

Definition
  • congestive heart failure + atrial fibrillation or enlarged/dysfunctional left ventricle 
  • cardiac glycoside 
  • inhibits Na+/K+ ATPase
  • direct effect: ↑ Na+ inside cell ➞ ↓ Ca2+ efflux out of cell ➞ ↑ intracellular Ca2+ ➞ ↑ interaction between actin + myosin ➞ ↑ cardiac contractility (strengthen output)
  • indirect effect: ↑ PSNS and ↓ SNS activity from improved circulation ➞ ↓ baroreceptor activation (↓ rate and how hard heart has to work)
  • therefore ↑ force and ↓ rate of contraction 
  • toxicities: arrhythmia (people with low K+) ➞ tachycardia and fibrillation, Quinidine reduces clearance, GI toxicities (anorexia, nausea, vomiting, and diarrhea) 
Term

Nitroglycerin

Definition
  • angina
  • nitrate goup converted to NO ➞ ↑cGMP ➞ relaxation of smooth muscle ➞ vasodilation (and other tissues ie. bronchioles)
  • effects = ↓ venous return, ↓ PVR, dilation of coronary arteries ➞ ↓ O2 requirements and ↑ O2 delivery
  • toxicities: hypotension, tachycardia (baroreceptore reflex), headaches, and when used with sildenafil
Term

Quinidine

Definition
  • arrhythmia (all types)
  • Na+ channel blocker
  • prolongs Na+ channel in inactive phase ➞ subsequent stimulation of Na+ is delayed
  • long-term treatment
Term

Lidocaine

Definition
  • arrhythmia 
  • ventricular tachycardia/fibrillation
  • emergency situations
  • same mechanism as Quinidine
Term

Amiodarone

Definition
  • arrhythmias
  • K+ channel blocker
  • prolongs action potential duration ➞ delays time for next AP
  • also effects β-receptors + Na+/Ca+ channels
  • most common for atrial fibrillations, ventricular tachycardia)
Term

Donepezil

Definition
  • mild-moderate Alzheimer’s 
  • Acetylcholine esterase inhibitor 
  • inhibit breakdown of ACh
  • side effects = similar to peripheral acting AChE inhibitors (primarily autonomic)
Term

L-Dopa (levodopa)

Definition
  • precursor to dopamine, norepinephrine, epinephrine
  • can ↑ dopamine levels in brain 
  • converted to dopamine by L-amino acid dexarboxylase (DDC)
  • side effects = hypotension, arrhythmias, nausea, disturbed respiration, hair loss, confusion, extreme emotions (ie. anxiety), insomina, narcolepsy
Term

Ropinirole

Definition
  • Parkinsons
  • dopamine agonist (D2, D3, D4 receptors)
Term

Selegiline, deprenyl

Definition
  • Parkinsons
  • MAO inhibitor
Term

Benztropine

Definition
  • Parkinsons
  • antimuscarinic  
Term

Haloperidol

Definition
  • psychosis
  • butyrophenone derivative 
  • receptor antagonist: D2 > α1 > D4 > 5-HT2a > D1 > H1 
  • side effects: parkinson-like symptoms (D2 blockade), hypotension (α1 blockade)
Term

Olanzapine

Definition
  • psychosis
  • atypical receptor antagonist: 5-HT2a > H1 > D4 > D2 > α1 > D1
  • side effects: sedation (5-HT2a blockade)
Term

Lithium

Definition
  • bipolar (most effective against mania)
  • may ↑ serotonin and ↓ NE + dopamine neurotransmission
  • lithium ➞ ↓ in precursors for IP2 and DAG synthesis ➞ ↓ IP3 + DAG when receptors linked to second messengers are activated (ie. muscarinic, α1, 5-HT2a receptors)
Term

Imipramine

Definition
  • depression
  • tricyclic antidepressant 
  • ↓ NE and serotonin re-uptake
  • adverse effects b/c = blocks cardiac sodium channels and is antagonist at muscarinic, histaminic, and α1 receptors
Term

Bupropion

Definition
  • depression
  • weak inhibitor of re-uptake and stimulates release of NE and dopamine
  • doesnt block histaminic, adrenergic, or muscarinic receptors
  • increases dopamine levels (not good in psychosis)
Term

Fluoxetine (Prozac)

Definition
  • depression, anxiety, OCD, bulemia
  • most widely prescribed
  • serotonin re-uptake inhibitor 
  • side effect: insomnia, sexual dysfunction, ↑ suicide rates in children, inhibits CYP2D6 (overdose when taken with other antidepressants)
Term

Phenelzine

Definition
  • depression
  • MAO inhibitor
  • not selective for MAO-A or MAO-B therefore ↑ NE, serotinin, and dopamine
  • only used when tricyclic don’t work 
  • no significant side-effects when taken on their own
  • when taken with a tyarmine-containing food or with CNS stimulants ➞ hypertensive crisis
  • do not take with any seroternergic agents (SSRIs, SNRIs, tricyclics) ➞ serotonin syndrome 
  • sympatheticomimetics contradicted in people taking MAOIs
Term

Diazepam (Valium)

Definition
  • anxiety, ethanol withdrawal
  • a benzodiazepine
  • all metabolites are active
  • enhances GABA neurotransmission by binding to GABAa receptor at different site and ↑ binding frequency of GABA-mediated opening of Cl- channel
  • enhance Cl- conductance ➞ ↑ inhibition of many neurons in many brain regions
Term

Phenobarbital

Definition
  • anxiety
  • a barbiturate
  • enhances GABA neurotransmission by binding GABAa at different site and ↑ duration of opening of GABA-mediated Cl- channels
  • at high doses can directly activate GABAa and inhibit glutamate receptors and high-frequency sodium channels (lower therapeutic margin)
  • also ↑expression of some cytochrome P450 enzymes
Term

Ethanol

Definition
  • a sedative-hypnotic
  • ↓ membrane excitability, ↑GABAa, ↓NMDA activation ➞ dose-dependent CNS depression
  • also: ↓ myocardial contractility, ↓ anxiety, slurred speech, impaired judgment 
  • toxicicity: CNS and respiratory depression
  • chronic use: fatty liver ➞ hepatitis ➞ cirrhosis ➞ liver failure, pancreatitis, gastritis, malnutrition
Term

Methanol

Definition
  • metabolizes ➞ formaldehyde ➞ formic acid
  • formic acid accumulation causes blindness
  • treat with ethanol (compete for alcohol dehydrogenase)
Term

Heroine

Definition
  • drug of abuse
  • opioid
  • presynaptic: binds to μ receptor linked to G-protein ➞ ↓ Ca+ ➞ ↓ release of neurotransmitters (GABA and glutamate)
  • postynaptic: binds to μ receptor ➞ ↑ K+ efflux ➞ inhibits postsynaptic renurons (more negative and harder to activate)
  • overdoes: respiratory depression ➞ coma ➞ death
  • methadon and chlonidine to treat withdrawal
Term

Cocaine

Definition
  • drugs of abuse
  • stimulant
  • highly addictive
  • ↓ re-uptake of NE, dopamine, and serotonin ➞ ↑ alertness and euphoria
  • side-effects: psychosis, delusions, excess SNS activity
  • overdoes: intracranial hemorrhage, stroke, seizure, arrhythmia, heart attack, hyperthermia, coma, death
Term

 Amphetamines

Definition
  • drug of abuse
  • stimulant
  • ↑ release of NE, dopamine, and serotonin ➞ ↑ alertness and euphoria
  • side-effects: psychosis, delusions, excess SNS activity
  • overdose: hyperthermia, serotonin syndrome, seizures, neuronal damage
Term

LSD (lysergic acid diethylamide), mescaline, psilocybin

Definition
  • drug of abuse
  • 5-HT2a partial agonist 
  • causes visual illusions and perceptual distortion
  • side effects: panic, psychosis, strong uterine contractions
Term

Phencyclindine (PCP)

Definition
  • drug of abuse
  • NMDA receptor antagonist
  • causes visual illusions and perceptual distortion
  • side effects: panic, psychosis
  • can be fatal in overdose 

 

Term

Marijuana, Hashish

Definition
  • drug of abuse, cancer, glaucoma, AIDS
  • THC binds cannaboid receptor (CB1 and CB2) linked to G-protein ➞ inhibits GABA or glutamate release
  • initial effect: euphoria, laughter, altered sense of time
  • secondary effect: relaxation, introspection, ↓ reaction time, ↓ learning/memory
  • side effects: can causes paranoia, anxiety, hallucinations
  • chronic: bronchitis, lung cancer 
Term

Dexmedetomidine

Definition
  • sedative and analgesic
  • α-2 agonists
  • stimulate α2 receptor ➞ open K+ channels ➞ inhibit neurotransmitter release in brain
  • causes: sedation, analgesia, hypotension, muscle relaxing, ↓ O2 exchange

 

 

 

Term

 Diazepam (Valium)

Definition
  • sedative-hypnotic, muscle relaxant
  • benzodiazepine
  • enhances GABA neurotransmission by binding to GABAa receptor at different site and ↑ binding frequency of GAMA-mediated opening of Cl- channel
  • enhance Cl- conductance ➞ ↑ inhibition of many neurons in many brain region
  • little effect on cadiovascular system and little respiratory depressant at therapeutic doses
  • side effect: drowsiness and confusion, CNS depression with alcohol use
  • adverse effects reversed by flumazenil (GABAa antagonist)
Term

Fentanyl

Definition
  • analgesic, sedative, cough suppression
  • opioid
  • stimulate pre-synaptic μ-opioid receptor in CNS ➞ inhibits GABA and glutamate release ➞ intense analgesia
  • side effects: constipation, nausea, urine retension, dose-dependent resp depression (death in overdose)
Term

Pentazocine

Definition
  • good analgesia but weaker effect at μ receptor (partial agonist)
  • opioid
Term

Naloxone

Definition
  • reverse opioid overdose, opioid effects after surgery, or for shocky patients 
  • opioid receptor antagonist
Term

Etorphine (M-99)

Definition
  • 1000-8000 X more potent than morphine 
  • opioid
  • used in wild-life
  • reversal agent = M5050
Term

Thiopental Sodium

Definition
  • induction agent and short term anesthesia
  • barbituate 
  • enhances GABA neurotransmission by binding GABAa at different site and ↑ duration of opening of GABA-mediated Cl- channels
  • at high doses can directly activate GABAa and inhibit glutamate receptors and high-frequency sodium channels (lower therapeutic margin)
  • does-dependent CNS but partial does causes excitement, less smooth recovery (esp if multiple doses)
  • effects: does-dependent resp depression, 30 second apnea,  hypotension, and extravascular damage
Term

Propofol

Definition
  • induction agent and short procedures
  • facilitates effect of GABA at GABAa in brain ➞ inhibits action potentials
  • smooth induction without excitement stage, rapid smooth recovery
  • adverse effects: dose-dendent resp depression, 60 second apnea, hypotension, diarrhea
Term

Ketamine

Definition
  • dissociative anasthetic and moderate analgesic
  • inhibits NMDA and GABA 
  • inhibits perception of signals associated with senses without totally abolishing consciousness
  • dissociative = open eyes, swallow, can hear, intense muscle rigidity, hallucinations, disconnected from surroundings and pain 
  • adverse effects: hypo- or hyperthermia, mood alterations, floating, vivid dreams, hallucinations, ↑ BP, minimal resp depression, can precipitate seizures, excitement if used alone
Term

Halothane

Definition
  • inhaled anesthetic
  • halogenate hydrocarbon
  • facilitates GABA at low concentrations and directly activates GABA receptors at high concentrations ➞ opens Cl- channels ➞ inhibits APs
  • adverse effects: liver damage (25% metabolism), ↓ CO + EP release + ↑ sensitivity to EP ➞ arrhythmias, hypothermia, malignant hyperthermia (inherited disorder)

 

Term

Isoflurane

Definition
  • inhaled anesthetic
  • halogenate hydrocarbon
  • facilitates GABA at low concentrations and directly activates GABA receptors at high concentrations ➞ opens Cl- channels ➞ inhibits APs
  • only 0.2% metabolized and low solubility in tissues ➞ less hepatic damage, less depression of CO, less potenet than halothane
  • adverse effects: dose-dependent ↓ in BP and bad odour
Term

Sevoflurane

Definition
  • inhaled anesthetic
  • halogenate hydrocarbon
  • facilitates GABA at low concentrations and directly activates GABA receptors at high concentrations ➞ opens Cl- channels ➞ inhibits APs
  • less odour and even less soluble in tissues than isoflurane but slightly more metabolized 
Term

Nitrous Oxide (N2O)

Definition
  • inhalant analgesic but not anesthetic
  • weak CNS depressant 
  • used to decrease amount of other inhalants needed and increase speed of gas anesthetic uptake 
  • no respiratory depression and little cardiovascular effects 
  • can cause toxicity (rapid uptake of other inhalants), gas pockets in GI, and hypoxia
Term

Atracarium

Definition
  • non-depolarizing neuromuscular blocker
  • competitive antagonist of AChRs (Nm)➞ intense relaxation or paralysis of voluntary muscle (dose-dependent)
  • prevents eye movement during ocular surgery
  • rapid reversal with AChEs (neostigmine, edrophenium)
  • adverse effects: can trigger histamine release, metabolized to laudacarium and can trigger seizures
  • now use lisatracarium (less adverse effects)
Term

Local Anesthetics

Definition
  • bind receptor on cytoplasmic surface of voltage-sensitive Na+ channels and block pore ➞ Na+ cant enter cell ➞ inhibits APs in axons
  • small fibers (ie pain) are blocked at lower concentrations ➞ motor fibers blocked last 
  • adverse effects: dose-dependent drowsiness ➞ excitations (seizures), ↓ excitability of myocardium ➞ AV block, arrhythmias, high concentrations = cardiac arrest, when with vasoconstrictor (ie. EP) ➞slow delayed healing and removal of drug ➞ prolongs action and doubles duration (toxicity)
Term

 Lidocaine

Definition
  • local anesthetic, arrhythmia (ventricular tachycardia/fibrillation)
  • various administrations
  • overdose = drowsiness or seizures ➞ muscle twitching and possibly cardiac arrest ➞ death
  • emergency situations
  • same mechanism as quinidine
Term

Bupivacaine

Definition
  • local anesthetic
  • slower onset but greater duration 
  • greater CVS toxicity
Term

 Levobupivacaine

Definition
  • local anesthetic 
  • S-enantomer of Bupivacaine
  • doesnt distribute to CNS and heart ➞ less CVS toxicities
Term

 Proparacaine

Definition
  • local anesthetic 
  • least irritating for eye
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