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X Pharmacology > Exam 1 Drugs > Flashcards

Exam 1 Drugs Flashcards

1
Q

What disease is copper toxicity associated with?

A

Wilson’s disease, body cannot eliminate copper and accumulates in tissue

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2
Q

Dimercaprol (BAL in Oil)

A

Chelator of arsenic mainly (also gold, mercury and acute lead)

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3
Q

Penicillamine (Cuprimine)

A

Chelator for copper poisoning

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4
Q

Deferoxamine (Desferal)

A

Chelator for iron poisoning

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5
Q

Calcium disodium edetate (Calcium Disodium Versenate)

A

Chelator for lead poisoning

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6
Q

What targets GPCRs?

A

CNS and autonomic drugs, cardiovascular drugs

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7
Q

What targets voltage-gated ion channels?

A

Local anesthetics, anticonvulsants (hydrophobic interactions because lipid soluble)

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8
Q

What targets ligand-gated ion channels?

A

Nicotine, benzodiazepenes

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9
Q

What targets intracellular receptors?

A

Corticosteroids, sex steroids, hormones (lipid soluble ligands)

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10
Q

What targets enzymes?

A

MAO inhibitors, cholinesterase inhibitors (covalent binding)

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11
Q

What targets transport proteins (DAT, SERT)?

A

Antidepressants

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12
Q

What targets nucleic acids?

A

Anticancer and antiviral drugs

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13
Q

Warfarin

A

Small therapeutic index (much riskier)

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14
Q

Penicillin

A

Large therapeutic index (much safer drug)

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15
Q

Aspirin

A

Participates in irreversible covalent binding

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16
Q

Epinephrine and histamine (what else does epinephrine do on its own?)

A

Physiological/functional antagonism can reverse a fall in blood pressure produced by histamine with epinephrine, both stimulate Gs and activate cAMP, epi can also stimulate Gi and inhibit cAMP

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17
Q

Phenobarbitol/barbiturates

A

Acts on GABA receptor to increase Cl- flow into the cell (synergism with ethanol)

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18
Q

Ethanol

A

Acts on GABA receptor to increase Cl- flow into the cell (synergism with barbiturates)

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19
Q

Drugs that are an example of pharmacokinetic tolerance

A

Barbiturates, ethanol, warfarin

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20
Q

What are 2 drugs that exhibit synergism on the depression of the CNS?

A

Diazepam plus ethanol

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21
Q

What is the relationship between warfarin and phenytoin?

A

These drugs compete for the same plasma binding sites so the dose of warfarin must be decreased in patients that take phenytoin (an anticonvulsant)

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22
Q

What is the overextension-type toxicity of aspirin, warfarin and heparin?

A

Hemorrhage

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23
Q

What is the organ directed toxicity of acetaminophen?

A

Hepatotoxicity

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24
Q

What are the organ directed toxic affects of warfarin?

A

Teratogenic affects so the placenta and therefore the baby are affected

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25
What is the effect of succinylcholine on patients with abnormal serum cholinesterase?
It is used to paralyze the muscles and it will cause a much longer recovery time of the paralysis (deficiency of metabolic enzymes leading to enhanced drug effects)
26
Codeine
Very weak analgesic so it must be metabolized to morphine, this metabolism is mediated by CYP450 2D6 (so if patient has a deficiency in this then they will not have the pain relief)
27
Where is aspirin absorbed?
In the stomach (weak acid)
28
Describe the mechanism of elimination of ethanol
Zero-order elimination where a constant amount is eliminated over time
29
Metabolites of diazepam
Nordiazepam (active) and oxazepam (mildly toxic), cleared very slowly
30
Metabolites of acetaminophen
N-acetyl-p-benzo-quinone imine (toxic)
31
How does ethanol affect acetaminophen?
It induces acetaminophen metabolism through CYP2E1 which increases the amount of drug in the toxic pathway
32
Isoniazid metabolism
Phase II (acetylation by n-acetylcysteine) occurs before Phase I (hydrolysis) and this results in toxic metabolites due to the acetylation of toxic metabolites, involved with n-acetyl transferase (phase II)
33
Mechanism of toxicity of nicotine
Interference with receptor-ligand interactions
34
Mechanism of toxicity of local anesthetics
Interference with membrane function
35
Mechanism of toxicity of MPTP
Toxicity from selective cell loss
36
Mechanism of toxicity of carcinogens
Non-lethal alterations in somatic cells
37
Mechanism of toxicity of dioxins
Interference with cellular TFs
38
Mechanism of toxicity of acetaminophen
Induction of programmed cell death
39
What compounds bind directly to cellular components leading to cell death?
CO, cyanide and lead
40
What compound undergoes redox cycling in presence of O2 to form ROS
Paraquat
41
What does activated charcoal do?
Adsorbs many toxins as a treatment of acute poisoning
42
What does ammonium chloride do?
Acidifies urine (bases) to enhance elimination
43
What does sodium bicarbonate do?
Alkalinizes urine (acids) to enhance elimination
44
Acetylcysteine
Used in acetaminophen poisoning to inactivate toxins
45
Atropine
Antidote for cholinesterase inhibitor poisons (OPs)
46
Cyanide antidote examples
Sodium nitrite, Na thiosulfate, amyl nitrite
47
Ethanol as a poison treatment
Used in methanol or ethylene glycol poisoning
48
Fomepizole
Antidote used in ethylene glycol poisoning
49
Bleach mechanism of poisoning (NO)
Causes oxidative stress with symptoms of severe irritation, hypotension, delirium or coma
50
Treatment of bleach poisoning
Remove from skin by flooding with water and then used milk, melted ice cream or beaten eggs
51
Ethylene glycol mechanism of poisoning
Converted to oxalic acid by alcohol dehydrogenase, which alters calcium homeostasis and causes CNS depression and kidney damage due to calcium oxalate crystals
52
Treatment of ethylene glycol poisoning
Gastric lavage, give ethanol IV as antidote or fomepizole
53
Botulinus toxin mechanism of poisoning
Inhibits release of Ach and causes vomiting, double vision and muscular paralysis
54
Treatment of botulinus toxin poisoning
Emesis/lavage/cathartic, draw blood to measure toxin concentration and give equine trivalent antitoxin (ABE)
55
Mechanism of organophosphate (parathion, malathion) poisoning
Irreversible cholinesterase inhibitors (because bind biomolecules)
56
Main symptoms of organophosphate poisoning
SLUD (salivation, lacrimation, urination and defecation)
57
Treatment of organophosphate poisoning
Atropine to block cholinergic effects, gastric lavage or emesis if recent ingestion, 2-PAM to reactivate acetylcholinesterase enzyme
58
Mechanism of organochlorine pesticide poisoning (DDT, dieldrin)
Bioaccumulation and interfere with inactivation of sodium channels to enhance neuron excitability causing rapid repetitive firing causing twitches/convulsions
59
Mechanism of chlorophenoxy compound poisoning
Need high doses to produce toxicity, agonist for aryl hydrocarbon receptor and induces gene expression
60
Mechanism of paraquat poisoning (NO)
Causes oxidative stress because it undergoes redox cycling and causes oxidative injury to the lungs
61
Treatment for paraquat poisoning
Lavage, cathartics, charcoal and prolonged observation
62
Mechanism of carbon tetrachloride (chloroform)
Metabolized by CYP450 to free radicals and the free-radical induced lipid peroxidation causes increase in intracellular Ca2+ leading to apoptotic death
63
Mechanism of mineral acids
Oxidative stress
64
Treatment for mineral acid poisoning
DO NOT USE GASTRIC LAVAGE OR EMETIC COMPOUDS, dilute with water and reduce pain, non-specific antidote is milk of magnesia
65
Mechanism of arsenic poisoning
Binds SH groups on metabolic enzymes, increases oxidative stress and alters gene expression
66
Symptoms of acute poisoning of arsenic
GI effects, CNS effects, ventricular arrhythmias, kidney tubular damage
67
Symptoms of chronic arsenic poisoning
Polyneuritis, nephritis, cardiac failure, cirrhosis of liver
68
Treatment for arsenic poisoning
Lavage/emesis and Dimercaprol
69
Treatment for lead poisoning
Chelation (edetate calcium disodium), forms organic lead which is likely to cross BBB (not as toxic to body but will affect brain)
70
Mechanism of iron poisoning (NO)
Oxidative injury
71
Treatment for iron poisoning
Lavage only within first hour, administer deferoxamine orally and parenterally
72
Mechanism of copper poisoning
Redox cycles, increases oxidative stress
73
Kayser-Fleischer rings
Copper deposits in the cornea seen in copper poisoning
74
Mechanism of asbestos poisoning
Redox cycles, increases oxidative stress, chronic inflammatory action, can increase delivery and activation of carcinogenic chemicals
75
What color is carboxyhemoglobin?
Cherry red
76
Mechanism of CO poisoning
CO has greater affinity than O2 for hemoglobin and forms carboxyhemoglobin, impairs ability of oxyhemoglobin to transport O2
77
Mechanism of cyanide poisoning
Complexes with ferric ion of cytochrome oxidase, produces cellular anoxia by inhibiting oxygen utilization in the mitochondria
78
Treatment for cyanide poisoning
Cyanide antidote (administer sodium nitrite or amyl nitrite), sodium thiosulfate is given after nitrite administration, rhodanese and then respiration with 100% O2
79
What is the mechanism of the cyanide antidote?
Induces methemoglobinnemia which binds free CN-
80
What is rhodanese?
Mitochondrial enzyme that converts CN- to SCN
81
Inducer of CYP450
Ethanol
82
Codeine and aspirin
Summation effect on pain
83
Tachyphylaxis
Rapid development of tolerance as seen in amphetamines
84
Example of synergism
Depression of CNS by diazepam and ethanole
85
Overextension toxicity of sedative hypnotics
Excessive CNS depression
86
Common drugs that produce hypersensitivity reactions
Penicillin/heparin (highly charged) or isoniazid/hydralazine in slow acetylators (long half life)
87
Drugs with a low volume of distribution
Heparin/warfarin
88
Drugs with a high volume of distribution
Acetaminophen/propranolol
89
Reductive Phase I reaction affecting Warfarin
Inactivated by CYP2A6
90
Effect of functional 2D6 genes on nortryiptyline metabolism
Lower number of genes leads to higher plasma concentration of the drug
91
What does Fluoxetine (Prozac) inhibit?
CYP2D6 (codeine or oxycodone)
92
Relationship between Abacavir and HLA
HLA is involved in hypersensitivity reactions like SJS, pts with HLA-B*5701 variant are much more likely to be hypersensitive to abacavir (which is an anticonvulsant)
93
Drugs used for oxidation defect of CYP2D6
Codeine, debrisoquin (antihypertensive) and nortriptyline (antidepressant)

X Pharmacology (1 decks)

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