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Pharmacology > Pharm Unit 2 > Flashcards

Pharm Unit 2 Flashcards

1
Q

Tyrosine Hydroxylase

A

Rate limiting step in dopamine production; produces DOPA from tyrosine

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2
Q

Metyrosine

A

Binds to tyrosine hydroxylase and outcompletes tyrosine for binding; not formed into DOPA; leads to depletion of DOPA and dopamine

Can be used to reduce BP (less dopamine = less conversion to NE = less adrenergic stimulation

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3
Q

L-DOPA

A

Precursor of dopamine, used to treat Parkinson’s Disease where dopaminergic neurons are lost. Dopamine loading can have adverse cardiovascular effects due to conversion of dopamine to NE

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4
Q

Carbidopa

A

Blocks conversion of L-DOPA to dopamine.
Does not cross BBB.
Reduces cardiovascular side effects of dopamine in peripheral adrenergic nerves but maintains dopamine concentrations in CNS

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5
Q

Reserpine

A

Blocks vesicular monoamine transporter, leads to depletion of monoamines (NE, dopamine, serotonin)
CAN CROSS BBB AND BLOCK MONOAMINE UPTAKE IN THE CNS which may contribute to depression.
Also used to treat hypertension by blocking NE vesicular uptake.

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6
Q

Dopamine beta-hydroxylase

A

Converts dopamine to NE, found in adrenergic nerves.

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7
Q

Bretylium

A

Inhibits excitability of nerve terminal membrane and fusion of synaptic vesicle with plasma membrane.
INHIBITS NE RELEASE - used for treating emergent arrhytmias

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8
Q

Cocaine

A

Inhibits reuptake of monoamines such as NE, dopamine, and serotonin

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9
Q

Tri-cyclic antidepressants

A

Block reuptake of several monoamines

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10
Q

SSRIs

A

Block reuptake of serotonin; increase concentration of serotonin in synapse

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11
Q

Phenylephrine

A

Synthetic drugs used to activate adrenergic receptors; resistant to degradation by COMT and has a longer resulting half-life

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12
Q

MAOIs

A

Inhibit monoamine oxidase in the cytosol, leads to greater cytoplasmic catecholamine concentration
As NE accumulates, the transporter reverses direction and expels NE into the synapse

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13
Q

Tyramine

A

Normally undergoes large first pass metabolism but accumulates in the cytoplasm when MAOIs are administered
Outcompetes NE for vesicular transport, leading to more extrusion of NE into synapse
Can lead to hypertensive crisis due to NE stimulating peripheral alpha-1 receptors and causing vasoconstriction

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14
Q

Naloxone

A

Small lipophilic molecule used to treat opiate overdose

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15
Q

Naltrexone

A

Longer half life than naloxone, used to treat opiate addiction and alcoholism

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16
Q

Alpha-1 receptor

A

Stimulates vascular smooth muscle contraction

Causes contraction of pupillary dilator muscle

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17
Q

Beta-1 receptor

A

Found in the heart; stimulates rate and force of contraction

Also found on juxtaglomerular cells - activation stimulates renin release

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18
Q

Beta-2 receptor

A

Mediates smooth muscle relaxation (respiratory, uterine, vascular)
Stimulated in treatment of asthma and COPD
Somatic motor nerve terminals express this receptor - activation of receptor may facilitate ACh release in skeletal muscle, causing tremors

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19
Q

Dopamine-1 receptor

A

Found in smooth muscle that lines blood vessels that perfuse kidney and splanchnic organs - activation causes vasodilation
At higher concentrations, dopamine activates adrenergic receptors - leads to vasoconstriction

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20
Q

Epinephrine

A

Mechanism of action - stimulates all four adrenergic receptors in dose-dependent manner
Indications - anaphylaxis, cardiac arrest, bronchospasm (beta-2 receptor)
Contraindications - later term pregnancy
Toxicity - Arrhythmia (beta-1 receptor stimulation)
Physiological effects - increased cardiac output and lower diastolic BP in low dose, elevated TPR and increased CO in high doses; bronchodilation (beta-2 receptor); decreased bronchial secretions (alpha-1 receptor)

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21
Q

Norepinephrine

A

Binds all adrenergic receptors except for beta-2
Physiological effects - increased cardiac output (beta-1); increased TPR (alpha-1 and alpha-2); decreased heart rate (baroreflex due to increased diastolic BP); overall increased mean arterial pressure
Indications - limited to shock (promotes vasoconstriction)
Contraindications - pre-existing vasoconstriction or ischemia
Toxicity - ischemia

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22
Q

Dopamine

A

At low doses stimulates dopamine and beta-1 receptor; at high doses also stimulates alpha-1 and alpha-2 receptors.
Physiological effects - low levels decrease TPR (D1 receptor) and increase CO (beta-1 receptor); high levels increase MAP and TPR (alpha-1, 2, beta-1)
Indications - cardiogenic shock - increased HR and contractility (beta-1) and blood flow to kidney and splanchnics (D1)
Toxicity - low BP at low infusion rates (D1); ischemia at high infusion rates (alpha receptors)
Contraindications - tachycardia (beta-1 receptor); V-Fib

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23
Q

Isoproterenol

A

Non-selective beta agonist - binds both beta-1 and beta-2 receptor
Physiological effects - decrease TPR (beta-2); Increase CO (beta-1); decrease in MAP (beta-2); bronchodilation (beta-2); increased HR (baroreflex due to decreased diastolic pressure)
Indications - bradycardia promoting heart block when TPR is high
Contraindications - angina with arrhythmia
Toxicity - tachyarrhythmia (beta-1 activation)

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24
Q

Dobutamine

A

Prototype for selective beta-1 agonist (will bind beta-2 at high concentrations)
Physiological effects - increased cardiac output
Indications - short term for CHF or cardiogenic shock
Toxicity - arrhythmia (beta-1 receptor); hypotension (caused by dose that activates beta-2 receptor)

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25
Q

Terbutaline and albuterol

A

Beta-2 agonists but can bind beta-1 receptors at high concentrations
Physiological effects - bronchodilation and uterine relaxation
Indications - bronchospasm and treatment of obstructive airway disease
Toxicity - tachycardia (beta-1 receptor); muscle tremor (beta-2 receptor on somatic nerve terminals); tolerance (beta-2 - long term use can internalize receptors)

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26
Q

Phenylephrine (not subject to COMT degradation)

A

Selective alpha-1 receptor agonist
Physiological effects - Increase TPR and MAP; decrease HR (baroreflex due to increased BP); pupillary dilation; decreased bronchiole and sinus secretions
Indications - hypotension during anesthesia; SVT; mydriatic agent; nasal congestion
Toxicity - hypertension
Contraindications - hypertension; ventricular tachycardia

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27
Q

Clonidine

A

Selective alpha-2 receptor agonist
Indications - hypertension due to sympathetic activation (alpha-2 presynaptic binding causes decreased NE release)
Physiological effects - acutely increased BP due to alpha-2 receptors in vasculature; decreased sympathetic activation later leads to decreased alpha-1 and alpha-2 activation, reducing BP
Toxicity - dry mouth (inhibits sympathetic drive); hypertensive crisis (after acute withdrawal); sedation; bradycardia

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28
Q

Indirect acting sympathomimetics - definition and list

A

Increase activity of endogenous released agonists - these are releasing agents or reuptake inhibitors

Amphetamine (prototype)
Methylphenidate (dopamine reuptake inhibitor)
Ephedrine
Pseudoephedrine
Tyramine
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29
Q

Amphetamine

A

Binds to monoamine reuptake transporter and causes reversal of the transporter, leading to monoamine release in a calcium-independent manner
Physiological effects (same as NE) - increased TPR and diastolic BP; positive inotropic and chronotropic effects; increased systolic BP; CNS STIMULANT (increased NE, used for ADD); anorexia (increase dopamine)
Toxicity - tachycardia (beta-1 receptors)
Indications - ADD; narcolepsy; nasal congestion
Contraindications - hypertension; severe atherosclerosis (increase in BP can disrupt plaques); history of drug abuse; use of MAOIs within 2 weeks

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30
Q

Propranolol, nadolol, timolol

A

Non-selective beta blockers
Propranolol (prototype)
Nadolol - longer half life
Timolol - topally applied to eye - inhibits aqueous humor production
Indications - hypertension; angina (reduced oxygen requirements); glaucoma; early to moderate heart failure; arrhythmia; thyrotoxicosis (overactive thyroid stimulates sympathetic nervous system); anxiety
Physiological effects - decreased HR; decreased contractility; decreased renin release; reduced sympathetic activation; inhibition of aqueous humor production
Toxicity - bronchospasm; masks symptoms of hypoglycemia (beta-2 receptor); bradycardia
Contraindications - bronchospasms during asthma; sinus bradycardia; 2nd and 3rd degree heart block; cardiogenic shock

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31
Q

Metoprolol, atenolol, esmolol

A

Cardioselective beta blockers - block beta-2 receptor
Metoprolol crosses BBB while atenolol
Esmolol - short acting, reverses acute arrhythmia in emergency
Physiological effects - decreased HR; decreased contractility; decreased renin release; decreased sympathetic activation
Indications - hypertesion, angina, arrhythmia
Toxicity - hypotension, bradycardia
Contraindications - sinus bradycardia, 2nd and 3rd degree heart block, cardiogenic shock

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32
Q

Pancuronium

A

Prototypical non-depolarizing muscle relaxant
Antagonist of Nm channel
Longest half life of non-depolarizing muscle relaxants - renal elimination
Indications - important for patients who require mechanical ventilation for prolonged period of time
Specific side effects - muscarinic blockage (increased HR and CO)

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33
Q

Non-depolarizing muscle relaxants

A

Pancuronium, vecuronium, rocuronium, mivacurium
Indications - adjuvant to anesthesia during surgery; relaxation of larynx for ET intubation; relaxation of chest during mechanical ventilation
Side effects - non-analgesic; apnea
Interactions - INHALATION ANESTHETICS (enhance effect); ANTIBIOTICS (particularly aminoglycosides - enhance effect)
Antidote - ACE inhibitors; muscarinic blockers (glycopyrrolate)

34
Q

Vecuronium

A

Half life of roughly one hour

Primarily metabolized by the kidney

35
Q

Rocuronium

A

Half life of roughly one hour
Primarily metabolized by the liver
Side effect - can promote muscarinic blockade

36
Q

Mivacurium

A

Acts very rapidly, lasts for a few minutes
Metabolized solely by cholinesterase
Side effect - histamine release leads to allergic reaction (drug is short acting so allergic response is also short acting)

37
Q

Succinylcholine

A

Prototypical depolarizing muscle relaxant
Binds ACh receptor - leads to a single contraction, followed by fasciculations and flaccid paralysis
Short term leads to Phase I block, prolonged exposure leads to Phase II block
Treatment of Phase I block = time
Treatment of Phase II block = ACE inhibitors
More rapid onset than non-depolarizing agents
Degradation and metabolism mediated by plasma cholinesterase
Indications - ET intubation; suppression of muscle contraction during electroconvulsive therapy (short acting drug for short procedure)
Side effects - not analgesic; apnea; muscle pain (fasciculations); increased intraocular and intragastric pressure (fasciculations); stimulation of ganglionic nicotinic receptors; stimulation of muscarinic receptors in SA node at high concentrations (leads to arrhythmia and hypertension); HYPERKALEMIA
Contraindications - FAMILY HISTORY OF MALIGNANT HYPERTHERMIA; burns; major soft tissue injury; skeletal muscle myopathies

38
Q

Baclofen

A

Used to treat spasticity
Direct agonist of GABA-B receptors (expressed on excitatory 1a afferent nerve terminals)
MOA - inhibits neurotransmitter release (negatively coupled to adenylyl cyclase)
Physiological effect - reduces calcium influx at 1a afferent nerve terminal; reduces substance P in SC
Indication - spinal cord spasticity; MS
Toxicity - drowsiness

39
Q

Diazepam

A

Positive allosteric modulator of GABA-A receptor (opens chloride channel and leads to hyperpolarization of the membrane)
GABAergic neurons provide pre-synaptic inhibition of 1a afferents
Indications - MS; spinal spasticity
Toxicity - drowsiness; sedation
Contraindications - acute narrow-angle glaucoma; untreated open-angle glaucoma

40
Q

Tizanidine

A

Alpha-2 adrenergic agonist
Indications - MS; spinal spasticity
Toxicity - drowsiness; hypotension (alpha-2 pre-synaptic stimulation decreases NE release, less sympathetic stimulation)

41
Q

Dantrolene

A

Blocks calcium release from SR of skeletal muscle
Indications - spasticity; malignant hyperthermia
Toxicity - muscle weakness; sedation

42
Q

Buspirone

A

5-HT1a partial agonist
Indications - generalized anxiety disorder; off label use with SSRI for major depression
Side effects - may initially worsen anxiety

43
Q

Sumatriptan

A

5-HT1d agonist
Indication - prophylactic for migraine
Side effects - coronary vasoconstriction

44
Q

Fluoxetine, Sertraline

A

SSRIs
Indications - depression; PTSD; OCD
Side effects - sexual dysfunction; insomnia

45
Q

Trazadone

A

5-HT2A and 2C antagonist + SSRI
Indication - anxiety; depression
Side effects - suicidality early after initiation

46
Q

Risperidone

A

5-HT2A and 2C antagonist
Indications - Schizophrenia with psychosis
Side effects - weight gain and akathesia

47
Q

Ondansetron

A

5-HT3 receptor antagonist

Indication - decreases nausea and vomiting associated with chemotherapy

48
Q

Metoclopramide/Cisapride

A

5-HT4 receptor agonist, D2 antagonist

Indication - gastroparesis (low motility)

49
Q

Bromocriptine

A

D2 agonist

Indication - treatment of Parkinson’s disease

50
Q

Selegiline

A

MAO-B inhibitor
Indications - Parkinson’s disease at low doses; depression at high doses
Side effects - hypotension; hypertensive crisis
Contraindications - use of sympathomimetics

51
Q

Tolcapone

A

COMT inhibitor

Indication - treatment of Parkinson’s disease

52
Q

Haloperidol

A

D2 antagonist

Indications - treatment of acute psychosis

53
Q

Methylphenidate

A

Dopamine reuptake inhibitor
Indications - used to treat ADHD
Contraindications - TCA

54
Q

Morphine

A

Strong opioid
Indications - Pain in MI, sickle cell, surgical conditions, trauma, kidney stones
Side effects - constipation; addiction, tolerance; respiratory depression and asphyxia

55
Q

Meperidine

A

Strong opioid
Indications - relieves moderate to severe pain
Side effects - serotonin syndrome; seizure; dysphoria; tremor; respiratory depression

56
Q

Hydrocodone

A

Moderately strong opioid
Indications - treatment of moderate to severe pain; dry hacking associated with bronchitis
Side effects - constipation; respiratory depression; drowsiness; anxiety
Can be taken recreationally - causes mental numbness and euphoria

57
Q

Codeine

A

Moderately strong opioid
Indications - cough, diarrhea, IBS, narcolepsy
Side effects - euphoria; depression; constipation; erectile dysfunction

58
Q

Pentazocine

A

Agonist/antagonist drug
Exists in two enantiomers: (+) is a delta agonist; (-) is a kappa agonist and mu antagonist
Indication - relieves mild to moderate pain like in dental extraction
Side effects - weakly antagonizes analgesic effects of morphine and meperidine (antagonizes mu receptor)

59
Q

Methadone

A

Strong opioid
Mu and delta receptor agonist; antagonist of glutamate receptor and neuronal ACh receptor
Used to treat opioid addiction - lasts longer than other opiates, drug user relies less on other drugs and improves with time

60
Q

Naloxone

A

Antagonist for kappa and delta receptor - used to treat opioid overdose

61
Q

Methacholine

A

QNA; muscarinic agonist - fast acting
Uses - diagnosis of asthma - promotes bronchoconstriction (M3 receptor)
Toxicity - bronchoconstriction
Contraindication - beta blockade (need to administer beta-2 agonist to counteract methacholine toxicity)

62
Q

Carbachol

A

QNA; muscarinic agonist
Acts at both MUSCARINIC AND NICOTINIC RECEPTORS
Uses - topical miotic agent for ocular surgery and glaucoma; reduces intraocular pressure
Toxicity - excess muscarinic activation (brochoconstriction, reduced cardiac conduction (M2))

63
Q

Bethanecol

A

QNA; muscarinic agonist
Uses - post-op urinary retention, neurogenic bladder atony
Toxicity - bradycardia (M2), bronchoconstriction (M3)
Contraindications - asthma, bradycardia, peptic ulcer (stimulates GI motility and secretions)

64
Q

Pilocarpine

A

Tertiary amine; muscarinic agonist
Crosses BBB - has appreciable CNS effects
Uses - dry mouth associated with neck radiotherapy and Sjogren’s disease; open angle and acute angle-closure glaucoma
Toxicity - excessive muscarinic stimulation

65
Q

Neostigmine

A

Reversible cholinesterase inhibitor
Elicits effects primarily at Nm junction (increases muscle contractions)
Uses - myasthenia gravis; reversal of non-depolarizing neuromuscular blockade
Toxicity - muscarinic and nicotinic hyperactivation
Contraindications - intestinal obstruction (increased M3 activity - peristalsis)

66
Q

Edrophonium

A

Reversible cholinesterase inhibitor
Uses - diagnosis of myasthenia gravis, dose adjustment with neostigmine (if edrophonium worsens symptoms, use less neostigmine; if it improves symptoms, use more neostigmine)
Toxicity - bradycardia, cardiac standstill
Contraindications - intestinal blockade, urinary obstruction

67
Q

Physostigmine

A

Reversible cholinesterase inhibitor
Can cross BBB
Uses - antidote for muscarinic antagonist poisoning (atropine overdose)
Toxicity - convulsions, respiratory depression, CV depression

68
Q

Donepezil

A

ACE inhibitor
Can cross BBB
Used in treatment of Alzheimer’s disease

69
Q

Echothiophate

A

Irreversible cholinergic inhibitor
Uses - long term miosis in treatment of open angle glaucoma (aqueous humor production - sympathetic function; parasympathetics inhibit aqueous humor production, can be used to treat glaucoma)

70
Q

Effects and treatment of irreversible cholinesterase inhibitors

A

Typically irreversible cholinesterase inhibitors are organophosphates
Effects - DUMBBELS
Defecation, urination, miosis, bradycardia, bronchorrhea, emesis, lacrimation, salivation
Treatment - ventilation, suction oral secretions, administer muscarinic blocker (atropine), administer cholinesterase inducer (2-PAM)

71
Q

Atropine

A

Muscarinic antagonist
Uses - treatment for organophosphate poisoning; induction of mydriasis; reverse bradycardia of vagal origin; reverse GI hypermotility; treatment of bladder spasm

72
Q

Scopolamine

A

Muscarinic antagonist
Highly toxic, use in small doses
Uses - nausea and vomiting associated with motion sickness or chemotherapy
Toxicity - anti-muscarinic actions

73
Q

Glycopyrrolate

A

Muscaric antagonist
Uses - protects against excessive muscarinic effects of cholinesterase inhibitors; reverses neuromuscular blockade; pre-operative anti-saliogogue
Toxicity - can cause heat stroke due to inability to sweat in heat

74
Q

Propofol

A

GABA agonist
Uses - induction, maintenance, sedation, OR procedures
Effects - deacreases CMRO2; decreases intracranial pressure; venodilation; arteriolar dilation; apnea

75
Q

Thiopental

A

Barbiturate
Arterial vasoconstrictor - may cause ischemia
Puts brain to sleep - decreases CMRO2

76
Q

Ketamine

A

NMDA receptor antagonist
Dissociative agent used for induction
Bronchodilator - patient keeps breathing
Increases CMRO2, ICP, and blood flow to brain
Increases BP and HR
Side effects - bad dreams, salivation, twitching

77
Q

Etomidate

A

GABA receptor agonsit
Has the least cardiovascular side effects
Vasoconstrictor - decreases CMRO2
May lead to adrenal suppression and decreases body’s stress response

78
Q

Pindolol

A

Partial agonist beta blocker - beneficial when sympathetic activity is high
Effects - decreased BP: decreased contractility; decreased renin release; decreased sympathetic activation
Indications - hypertension
Toxicity - hypotension
Contraindications - sinus bradycardia, cardiogenic shock, 2nd and 3rd degree heart block

79
Q

Phentolamine and Phenoxybenzamine

A

Non-selective alpha antagonists
Phentolamine is reversible, phenoxybenzamine is not
Indications - hypertension associated with pheochromocytoma
Toxicity - prolonged hypotension; reflex tachycardia (binding of NE to beta-1)

80
Q

Prazosin, Doxazosin, Terazosin

A

Alpha-1 antagonists
Indications - BPH and hypertension
Toxicity - orthostatic hypotension

Pharmacology (5 decks)

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