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Pharmacotherapeutics I > Drugs > Flashcards

Drugs Flashcards

1
Q

Chloramphenicol

A

In neonates interferes with mitochondrial ribosomes and causes gray baby syndrome. Sx- poor feeding, decreased breathing, CV collapse, cyanosis, and death

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2
Q

Succinylcholine

A

short acting muscle relaxer used in surgery. Butyrylcholinesterase (BChE) hydrolysis of this creates a decreased rate of metabolism of succinylcholine resulting in prolonged paralysis after drug exposure.

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3
Q

N-acetyltransferase 2 (NAT2)

A

Catalyzes the acetylation (route of metabolism for specific drugs) of isoniazid, hydralazine, and procainamide. This does either slow or fast acetylators (slow=build up and fast = not working)

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4
Q

CYP2D6

A

Metabolizes metoprolol (lowers <3 rate), haloperidol (Antipsychotic), codeine, and fluoxetine (Depression)

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5
Q

Metoprolol

A

A beta blcoker used to decrease the heart rate. A poor metabolizer has potential toxicity with standard doses of this medication.

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6
Q

Codeine

A

Ineffective w/out metabolism by CYP2D6 to from the more potent opioid morphine. Normal codeine does not result in overdose.

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7
Q

Thiopurine S-Methyltransferase (TPMT)

A

Catalyzes the S-mehtylation of thiopurine drugs such as 6-mercaptopurine and azathiprine immunosuppressant agents (Used in CHEMO)

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8
Q

Zileuton

A

used for asthma by decreasing the airway inflammation by inhibitiing 5-lipoxygenase.

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9
Q

Warfarin

A

Metabolized predominately by CYP2C9. Warfarin’s target is viamin K epoxide reductase (an enzyme that is required for vitamin K dependant generation of clotting factors)

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10
Q

Abacavir

A

HIV medication that has an idiosyncratic reaction with HLA-B*5701 by inducing hypersensitivity.

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11
Q

Aminoglycoside Antibiotics

A

Gentamicin, tobromycin, amikacin, neomycin, and streptomycin. Must be administered via a parenteral route due to poor GI absorption. Very water soluble w/ poor distribution into adipose tissue. Clearance is almost entirely renal

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12
Q

Vancomycin

A

Antibiotic.
Poorly absorbed orally although useful in tx of C.diff with PO route. Systemic infections require parenteral dosing.
Increases levels/effects of aminglycosides- used for infections together.
Half life of 5-11 hrs.

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13
Q

Phenytoin

A

Absorption from oral route is slow.
Highly protein bound
Consider diseases that result in decreased serum albumin concentration such at burns, nephrotic syndrome, and renal failure.
An example of a P450 inducer
Moves from 1st order quickly to zero order occurring even at therapeutic levels

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14
Q

Valproic acid

A

Used as antiepileptic and as a mood stablizer.
Bioavailability 90% relative to IV dose
Saturable protein binding 80-90% free fraction.
Metabolism extensively hepatic via glucuronidation (conjugation)
Only p450 inhibitor (in antiepileptic class.
Relationship b/w dose and total valproate [ ] is not linear.
Draw levels 2-4 days of initiation to etermine total valproic acid.

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15
Q

Carbamazepine

A

Anti-epileptic
Slow absorption
Highly protein bound to plasma albumin and alpha1-acid glycoprotein.
Concamitant tx w/ valproate sodium results in higher free fraction
Eliminated primarily by metabolic route, one active metabolite, carbamazepine 10, 11 epoxide.
Metabolized primarily by CYP3A4
Induces own metabolism and goes from a long 1/2 life to a shorter one.
Steady state= 2-5 days

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16
Q

Warfarin

A 
Oral anticoagulant-rapid complete absoption.
Onset of action 24-72 hrs. 
Peak effect 5-7 days
Highly protein bound (99%)
Metabolism primarily by CYP2C9
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17
Q

Digoxin

A

Cardiac medication
Absorbed by passive non-saturable diffusion in SI.
Distribution phase lasts 6-8 hrs.
Large volume to distribution. After distribuiton you have a 70:1 in the heart vs. in the blood.
Very narrow therapeutic index

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18
Q

Epinephrine

A

Andrenergic Agonist
Interacts with both alpha and beta
Low dose- mainly beta effects (vasodilation); high dose- alpha effects (vasoconstriction
CV: + inotropic, + chronotropic- increased CO
Alpha effects- vasoconstricts arterioles
B2- vasodilates vessels to liver and skeletal muscle
Net result- increased SBP w/ slight decrease in DBP
Respiratory- bronchodilation of smooth muscle (B2)
Hyperglycemia-decreased insulin release (alpha2) increased glycogenesis, increased release of glucagon (B2)
Lypolysis B1

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19
Q

Epinephrine therapeutic uses

A

Emergent tx of asthma, glaucoma, anaphylaxis, w/local anesthetics to prolong DOA through vasoconstriction

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20
Q

Epinephrine ADRs

A

CNS- anxiety, fear, tension, HA, tremor, hemorrahage, increased BP, cerebral hemorrhage
CV-arrhythmias
Pulmonary edema

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21
Q

Norepinephrine

A

Adrenergic Agonist
At therapeutic doses alpha 1 and beta 1 receptors are afected
CV- vasoconstriction in periphery (including kidney) reulting in elevated BP, baroreceptor reflex: increase BP -> increased vagal activity stimulation baroreceptors causing bradycardia.
Tx use shock through vascular resistance, increase BP

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22
Q

Dopamine

A

Adrenergic Agonist
Low doses act predominately on D1 receptors in renal, mesenteric, and coronary vascular beds (vasodilation).
Higher doses a positive inotrope (action at beta1)
High doses- vasoconstriction via alpha 1 receptors
DOC for shock, at appropriate doses is useful in management of low CO associated with compromised renal function such as in severe CHF.

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23
Q

Methoxamine

A

Adrenergic Agonist
Alpha 1 selective agonist
Not used often but used to tx shock

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24
Q

Phenylephrine

A

Adrenergic Agonist
Alpha 1 selective agonist
Used like psuedofedrin, Topical constrict vascular smooth muscle in relief or nasal congestion
Not catechol derivative so substrate for COMT
Induces reflex bradycardia when given parenterally, raises BP due to vasoconstriction.

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25
Oxymetazoline
Adrenergic Agonist Alpha 1 selective agonist Topical, constrict vascular smooth muscle in relief of opthamic hyperemia.
26
Chlonidine
Adrenergic Agonist Alpha 2 selective agonist Lowers BP by suppressing sympathetic outflow ADR dry mouth and sedation
27
a-methyldopa
Adrenergic Agonist alpha 2 selective agonist Metabolized to a-methylnorepinephrine which is an a agonist in CNS to decrease sympathetic outflow
28
Gaunfacine
Adrenergic Agonist a-2 agonist in CNS to decrease sympathetic outflow ADR dry mouth and sedation
29
Isoproterernol
Adrenergic Agonist Nonspecific B agonist (acts at B1 and B2) CV: + inotropic and chronotropic effects (B1); vasodilation of arterioles of skeletal muscle (B2) Pulmonary- bronchodilation (B2) Uses- stimulates heart in emergencies
30
Dobutamine
Adrenergic Agonist B1 selective Increases cardiac rate and output, usted to increased CO in CHF, racemic mixture cancers out alpha
31
Albuterol, pirbuterol, terbutaline
Adrenergic Agonist- B2 selective | Short acting bronchodilators (less cardiac stimulation)
32
Salmeterol and formoterol
Adrenergic Agonist B2 selective agents B2 long acting bronchodilator
33
Amphetamine
Indirect adrenergic agonist | CNS stimulant, increases BP by alpha effect of vasculature, beta effect on heart
34
Ephedrine
Mixed action Alpha, beta, and CNS stimulant Use- nasal sprays due to local vasoconstrictor activity; urinary incontinence Long DOA
35
Phenoxybenzamine
Adrenergic antagonist Alpha blocker Irreversible, nonselective and noncompetitive block, tx of pheochromocytoma to preclude HTN crisis that can result from manipulating tissue.
36
Phentolamine
Adrenergic antagonist Alpha blocker | Competitive, nonselective block (alpha 1 and 2 response is more E being created and alpha 1 decreased vasoconstriction)
37
Prazosin, doxazosin, terazosin
Adrenergic antagonist Alpha blocker Selective alpha1 blocker- used for vasodilation Tx- hypertension, BPH, CHF by relaxing the arterial and venous smooth muscle and decreased PVR.
38
Tamsulosin
Adrenergic antagonist Alpha blocker Tx of BPH (benign prostate hyperplasia) Inhibitor of Alpha 1 receptor on smooth muscle of prostate (decreases tone of bladder neck and prostate and improves urine flow.)
39
Propranolol (prototype)
Adrenergic antagonist beta blocker Nonselective Uses- lowers BP, used to tx angina, cardiac arrhythmias, MI, glaucoma, prophylaxis for migraines Effects- lowers cardiac output (rate and force), prevents vasodilation, bronchoconstriction, increased Na retention, decreased glycogenolysis, and glucagon secretion
40
Timolol and nadolol
Adrenergic antagonist beta blocker Nonspecific beta blocker Uses- glaucoma and HTN
41
Acebutolol, atenolol, metoprolol, esmolol
Adrenergic antagonist beta blocker Preferentially blocks beta 1 receptors- cardioselective Eliminates unwanted bronchoconstriction, little effect of CHO- metabolims, or PVR Useful in hypertensive DM pt on insulin or oral hypoglycemics
42
Pindolol and acebutal
Adenergic antagonists w/ partial activity | Weakly stimulate B1 and B2. Used for HTN
43
labetolol and carvediol
Antagonists of alpha1 and beta 1&2 receptors. Peripheral vasodilation, dont alter lipid of glucose levels. Carvediol decreased lipid peroxidation and vascular wall thickening to benefit CHF Uses of labetolol- HTN, CHF, PIH, HTN emergenies -> rapidly lowers BP
44
Benzodiazepines
Midazolam, diazepam, alprozolam, chlorazepate, lorazepam, chlordiazepoxide, clonazepam, flurazepam, temazepam, triazolam, zolpidem Do not activate receptor in absence of GABA. Still require 2 GABA to bind then benzo makes it work better Highly selective, high affinity drugs that bind a single site on GABA receptor a1, a2, a3, or a5, and a y subunit. Potency is correlated to hydrophobicity Highly protein bound
45
Benzodiazepines
Admin via oral, transmucocal, IM and IV. Metabolized by CYP3A4 Used as sleep enhancers, anxiolytics, sedatives, antiepileptics, muscle relaers, and for the tx of ETOH withdrawl. ADRs related to therapeutic effects- amnesia Antagonist Flumazenil reverses effects High potential for development of tolerance, dependence, and addiction
46
Barbiturates
Butabarbital, butalbital, methohexital, pentobarbital, primidone, secobarbital, and thiopental. Affect CNS sites in spinal cord, brainstem, and the brain. Cause sedation, amnesia, and LOC by affecting GABA receptors, Spinal cord- relaxes muscles and suppressed reflexes
47
Anesthetic barbiturates
Ionotrophic GABA receptor Thiopental, pentobarbital, and methohexital Act as agonists at GABA-a and enhance the receptors response to GABA (dont not require the presence of GABA at receptors)
48
Phenobarbital
Anticonvulsant Barbiturates | Less direct agonist. Works for inhibiiton effects but does not cause the same amount of sedation as anesthetics.
49
Barbiturates
Oral or IV admin. Lipid solubility allows to enter CNS, termination effect depends on redistribution from CNS to highly profused areas. Extensive hepatic metabolism P450 and induce P450 enzymes
50
Etomidate and Propofol
Ionotrophic GABA receptor Used to enduce conscious sedation prior to surgery. Enhance activation of GABA-A and at high doses acts as an antagonist. INduce anesthesia in high enough doses
51
Baclofen
Metabatrophic GABA receptror GABA-B agonist Used to tx spacicity associated with motor neuron disease. Mild- oral absorbed slowly, primarily cleared in urine, no tolerance. Severe- intrathecal- peaks at 4 hours, and tolerance develops after 1-2 years Withdrawl can precipitate acute hypersensitivity, rhabdomylosis, pruritus, delerium, and fever.
52
Ethanol
Multiple targets including GABA-A and glutamate receptors
53
Chloral hydrate
originally used as anesthetic now used to commit crimes and to prevent memory
54
Gamma hydroxybutyric acid (GHB)
GABA isomer clinical use for narcolepsy, used for crime and date rape
55
Riluzole, memantine, amantadine
NMDA antagoists (block the glutamate receptor, blocks the damage from excitatory)
56
Riluzole
Blocks NA channels therby decreasing glutamate plus acts as an NMDA antagonist (neurodegenerative disease)
57
Memantine and amantadine
Non-competitive blocker of NMDA. Memantine- alzheimers, Amantadine decreases dyskinesia in parkinsons
58
Lamotrigine
Stabilizes inactivated state of Na channel reducing excitability and glutamate release Used in seizures.
59
Felbamate
One mechanism inhibit NMDA receptors- seizures.
60
Tiagabine
competitive inhibitor of GAT-1 | Used for epilepsy
61
Vigabatrin
inhibits GABA-T | used as an anticonvulsant
62
a-methyltyosine
inhibits tyrosine hydroxylase (first step in synthesis of catecholamines)
63
Reserpine
Blocks VMAT, transport of bioamines (NE, DA, 5-HT) from cytoplasm into storage vesicles.
64
Tyramine
Dietary amine usually meabolized by MAO in GI and liver. In patients with MAO inhibitors on board tyramine is absorbed, large amounts cause displacement of vesicular NE and non vesicular release leading to hypertensive crisis.
65
Guanethidine
Displaces NE in storage vesicles, leading to gradual depletion of NE. Will be destroyed by MOA and CTOA
66
Amephetamine
Displaces endogenous NE. Weak inhibitor of MAO. Blocks reuptake by NET and DAT Little agonist action at alpha and beta receptors, marked behavioral effects
67
Cocaine
potent inhibitor of NET, essentially eliminates catecholamine transport Used as a local anesthetic
68
Imipramine, Fluoxetine
SSRI selective seratonin R inhibitor. | Inhibits NET
69
Tricyclic Antidepressants
Blocks Na+/K+ ATPase, blocks NET | Precents reuptake of epinephrine/norepinephrine leading to an increased DOA.
70
Phenelzine
Inhibits MAO-A, increasing NE and 5-HT (Serotonin) content. | Inhibits metabolism of NE and seratonin
71
Selegiline
Inhibits MAO, increasing DA | Low doses used for tx of Parkinsons
72
Procaine, tetracaine, cocaine
Ester linked anesthetics Metabolized locally by tissue and plasma esterases Minutes with short DOA Eliminated via the kidney
73
Lidocaine, prilocaine, bupivicaine, articaine
Amide linked anesthetics Primarily P450 in the liver Metabolites eliminated via kidneys Longer DOA differing from drug to drug
74
Procaine
Ester based local anesthetic Short acting, low hydrophobicity- low potency Used for infiltration anesthesia and dental procedures Rapidly metabolize in plasma by cholinesterases One metabolite PABA.
75
Tetracaine
Ester based local anesthetic long acting, highly potent due to high hydrophobicity Metabolized by cholinesterase in plasma but slower effect than with procaine as it is slowly released from tissues in the blood. Spinal and topical anesthesia
76
Cocaine
Natural occurring Ester based local anesthetic Medium potency and DOA Inhibits catecholamine uptake peripherally and centerally= vasoconstriction and euphoria (cardiac toxicity) Ophthalmic and tropical anesthesia
77
Lidocaine and Prilocaine
Amide based Moderate hydrophobicity, large fraction of drug is in neutral form at physiologic pH= rapid onset, med DOA, and moderate potency Metabolism by live by P450 Used for peripheral nerve blocks, epidural, spinal, and topical anesthesia. Toxicities- CNS depression and cardiotoxicity
78
Prilocaine
vasoconstricive
79
Lidocaine
antiarrhythmic
80
Bupivicaine
Amide based long DOA and highly hydrophobic (high potency) Metabolized by live P450 R and S enatiomer Cardiac toxicity due to blocking Na channels in cardiac myocytes during systole but is slow to dissociate during diastole.
81
Articaine
Amide based Exhibits an ester group making it act differently Partially metabolized in the plasma by cholinesterase and in the liver by P450
82
Bethanechol- cholinergic agonist
Acts on receptors M1, M2, M3 Poor substrate for AchE Sites- smooth musculature of the bladder and GI Actions- increased intestinal motility and tone, and stimulates detrusor muscles of the bladder while the trigone and sphincter are relaxed causing expulsion of urine. Therapeutic action- stimulates atonic bladder in postpartum or postoperative urinary renention.
83
Bethanechol side effects
sweating, salivation, flushing, HPOTN, N/D, abd pain and bronchospasm.
84
Carbachol (carbamylcholine)
Poor substrate of AchE with DOA of as long as 1hr Action- M1, M2, M3 and wak nicotinic agonist-CV and GI systems- may first stimulate then depress, can also cause release of epinephrine for adrenal medulla by its nicotinic acitons. Therapeutics- used seldomly, sometimes as miotic for gluacoma
85
Carbachol (Carbamylcholine) adverse reactions
Little to no side effects when used in the eye
86
Methacholine
Muscarinic Receptor Drug Receptors- M1, M2, M3 Used as diagnostic challenge for bronchial hyperreactivity and asthmatic conditions
87
Pilocarpine
Muscarinic Receptor Drug Dominant muscarinic response at M1, M2, M3 Tertiary amine and less potent Action- rapid miosis and contraction of the ciliary muscle Therapeutic use- emergency lowering of the intraocular pressure of both narrow and wide-angle glaucoma.
88
Pilocarpine ADR
CNS effects, profuse sweating and salivation
89
Physostigmine
Indirect- acting cholinomimetic drug Glaucoma (miosis in the eye); increased intestinal and bladder motility, reverse CNS and cardiac effects of TCA (tricyclic antidepressant); reverse CNS effects of atropine. Action- amplifies effect of Ach
90
Neostigmine, pyridostigmine, edrophonium
Indirect- acting cholinomimetic drug Myasthenia gravis, helps w/ reversal of neuromuscular block Action- amplified effects of Ach, increased muscle strength.
91
Isoflurophate and echothiopate
Indirect- acting cholinomimetic drug Glaucoma (not the 1st line therapy Action- amplifies the effect of Ach
92
Pralidoxime
Cholinesterase reactivator that breaks bonds between drugs and enzymes if the enzyme has not aged.
93
Celecoxib (celebrex)
may cause an increased risk of serious cardiovascular thrombotic events, MI, and stroke which can be fatal
94
Isotertinoin (Accutane)
Contraindicated in pregnancy | Major human fetal abnormalities, spontaneous abortions, and premature death.
95
Nicotinic receptor drugs- antagonists
Curare, pancuronium, cisatracurium, atacurium, mvacurium, and succinylcholine

Pharmacotherapeutics I (23 decks)

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