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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
Terbutaline and albuterol
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)
26
Phenylephrine (not subject to COMT degradation)
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
27
Clonidine
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
28
Indirect acting sympathomimetics - definition and list
Increase activity of endogenous released agonists - these are releasing agents or reuptake inhibitors ``` Amphetamine (prototype) Methylphenidate (dopamine reuptake inhibitor) Ephedrine Pseudoephedrine Tyramine ```
29
Amphetamine
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
30
Propranolol, nadolol, timolol
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
31
Metoprolol, atenolol, esmolol
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
32
Pancuronium
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)
33
Non-depolarizing muscle relaxants
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
Vecuronium
Half life of roughly one hour | Primarily metabolized by the kidney
35
Rocuronium
Half life of roughly one hour Primarily metabolized by the liver Side effect - can promote muscarinic blockade
36
Mivacurium
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
Succinylcholine
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
Baclofen
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
Diazepam
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
Tizanidine
Alpha-2 adrenergic agonist Indications - MS; spinal spasticity Toxicity - drowsiness; hypotension (alpha-2 pre-synaptic stimulation decreases NE release, less sympathetic stimulation)
41
Dantrolene
Blocks calcium release from SR of skeletal muscle Indications - spasticity; malignant hyperthermia Toxicity - muscle weakness; sedation
42
Buspirone
5-HT1a partial agonist Indications - generalized anxiety disorder; off label use with SSRI for major depression Side effects - may initially worsen anxiety
43
Sumatriptan
5-HT1d agonist Indication - prophylactic for migraine Side effects - coronary vasoconstriction
44
Fluoxetine, Sertraline
SSRIs Indications - depression; PTSD; OCD Side effects - sexual dysfunction; insomnia
45
Trazadone
5-HT2A and 2C antagonist + SSRI Indication - anxiety; depression Side effects - suicidality early after initiation
46
Risperidone
5-HT2A and 2C antagonist Indications - Schizophrenia with psychosis Side effects - weight gain and akathesia
47
Ondansetron
5-HT3 receptor antagonist | Indication - decreases nausea and vomiting associated with chemotherapy
48
Metoclopramide/Cisapride
5-HT4 receptor agonist, D2 antagonist | Indication - gastroparesis (low motility)
49
Bromocriptine
D2 agonist | Indication - treatment of Parkinson's disease
50
Selegiline
MAO-B inhibitor Indications - Parkinson's disease at low doses; depression at high doses Side effects - hypotension; hypertensive crisis Contraindications - use of sympathomimetics
51
Tolcapone
COMT inhibitor | Indication - treatment of Parkinson's disease
52
Haloperidol
D2 antagonist | Indications - treatment of acute psychosis
53
Methylphenidate
Dopamine reuptake inhibitor Indications - used to treat ADHD Contraindications - TCA
54
Morphine
Strong opioid Indications - Pain in MI, sickle cell, surgical conditions, trauma, kidney stones Side effects - constipation; addiction, tolerance; respiratory depression and asphyxia
55
Meperidine
Strong opioid Indications - relieves moderate to severe pain Side effects - serotonin syndrome; seizure; dysphoria; tremor; respiratory depression
56
Hydrocodone
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
Codeine
Moderately strong opioid Indications - cough, diarrhea, IBS, narcolepsy Side effects - euphoria; depression; constipation; erectile dysfunction
58
Pentazocine
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
Methadone
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
Naloxone
Antagonist for kappa and delta receptor - used to treat opioid overdose
61
Methacholine
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
Carbachol
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
Bethanecol
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
Pilocarpine
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
Neostigmine
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
Edrophonium
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
Physostigmine
Reversible cholinesterase inhibitor Can cross BBB Uses - antidote for muscarinic antagonist poisoning (atropine overdose) Toxicity - convulsions, respiratory depression, CV depression
68
Donepezil
ACE inhibitor Can cross BBB Used in treatment of Alzheimer's disease
69
Echothiophate
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
Effects and treatment of irreversible cholinesterase inhibitors
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
Atropine
Muscarinic antagonist Uses - treatment for organophosphate poisoning; induction of mydriasis; reverse bradycardia of vagal origin; reverse GI hypermotility; treatment of bladder spasm
72
Scopolamine
Muscarinic antagonist Highly toxic, use in small doses Uses - nausea and vomiting associated with motion sickness or chemotherapy Toxicity - anti-muscarinic actions
73
Glycopyrrolate
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
Propofol
GABA agonist Uses - induction, maintenance, sedation, OR procedures Effects - deacreases CMRO2; decreases intracranial pressure; venodilation; arteriolar dilation; apnea
75
Thiopental
Barbiturate Arterial vasoconstrictor - may cause ischemia Puts brain to sleep - decreases CMRO2
76
Ketamine
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
Etomidate
GABA receptor agonsit Has the least cardiovascular side effects Vasoconstrictor - decreases CMRO2 May lead to adrenal suppression and decreases body's stress response
78
Pindolol
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
Phentolamine and Phenoxybenzamine
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
Prazosin, Doxazosin, Terazosin
Alpha-1 antagonists Indications - BPH and hypertension Toxicity - orthostatic hypotension

Pharmacology (5 decks)

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