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Step 1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Relationship between Km and affinity

A

Inversely related

Inc Km = Dec affinity
Dec Km = Inc affinity

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2
Q

Efficacy

A

the maximal effect a drug can produce (vmax)

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3
Q

Potency

A

the amount of drug needed for a given effect (the lower the amount needed, the more potent the drug)

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4
Q

Therapeutic index

A

measurement of drug safety

Safer drugs have a higher therapeutic index
More dangerous drugs have a narrow therapeutic index

Therapeutic index = Median toxic dose (TD50)/median effective dose (ED50)

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5
Q

Zero order elimination

A

rate of elimination is constant regardless of concentration – plasma concentration decreases linearly with time
• Ex. Alcohol, Phenytoin, Aspirin

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6
Q

First order elimination

A

rate of elimination is directly proportional to the drug concentration (constant fraction of drug eliminated per unit time)
• 99% of drugs are eliminated this way

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7
Q

Effect of liver and kidney disease on Vd

A

dec protein binding = inc Vd

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8
Q

Effect of liver and kidney disease on loading dose and maintenance dose

A

In renal or liver disease, maintenance dose decreases (due to dec CL) while loading dose remains the same

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9
Q

Overdose on an acidic drug

A

alkalinize the urine! Give patient sodium bicarb

Ex. Aspirin overdose

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10
Q

Overdose on a basic drug

A

acidify the urine! Give patient ammonium chloride

Ex. amphetamine overdose

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11
Q

Phase One drug metabolism

A

reduction, deamination, hydrolysis and oxidation with CYP450 – yield slightly polar water-soluble metabolites

CYP450 is located in zone III of the liver

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12
Q

Phase Two drug metabolism

A

reactions that involve addition (Conjugation) of subgroups to –OH, -NH2, and –SH functions on molecule (methylation, glucoronidation, acetylation, sulfation) – yields very polar, inactive metabolites

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13
Q

What is the goal of drug metabolism?

A

To decrease lipid solubility and make the drug more water soluble - -to increase excretion

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14
Q

What phase of drug metabolism do elderly patients lose first?

A

Phase I metabolism

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15
Q

What presdisposes people to drug induced lupus? Examples of drugs that can cause lupus like syndrome?

A

Patients who are slow acetylators (phase II drug metabolism in the liver) – there is a decreased rate of metabolism

o	Procainamide (class IA antiarrhythmic), Hydralazine (HTN emergency), Isoniazid (TB drug), TNF-a inhibitors (enteracept)
o	Antihistone antibodies: sensitive for drug-induced lupus
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16
Q

Effects of a competitive antagonist on an agonist?

A

Dec potency, no effect on efficacy

ex. Diazepam (agonist) and Flumazenil (competitive antagonist)

Can be overcome by increasing concentration of agonist substrate

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17
Q

Effects of a noncompetitive antagonist on an agonist?

A

causes a decrease in efficacy

ex. Norepinephrine (agonist) and phenoxybenzamine (noncompetitive antagonist)

Cannot be overcome by increasing agonist substrate concentration

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18
Q

Patient ingests rat poison, what should you give to treat them?

A

Rat poison = warfarin

give them fresh frozen plasma to reverse symptoms

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19
Q

Mechanism and uses of acetaminophen

A

reversibly inhibits COX
o Anti-pyretic, analgesic, but NOT ANTI-INFLAMMATORY
o Used instead of Aspirin in children to avoid Reye syndrome

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20
Q

Acetaminophen overdose

A

produces hepatic necrosis due to depletion of glutathione and formation of toxic byproducts in the liver

• N-acetylcysteine is the antidote – regenerates glutathione

21
Q

Cholinesterase inhibitor poisoning treatment

A

Atropine (CNS and PNS) and pralidoxine (PNS)

Atropine>Pralidoxine

22
Q

Benzodiazepine overdose treatment

A

Flumazenil (competitive antagonist)

23
Q

B blocker overdose treatment

A

Saline, atropine, glucagon

24
Q

Arsenic poisoning treatment

A

Dimercaprol (chelating agent)

25
Q

Amphetamine overdose treatment

A

Ammonium chloride (to acidify urine)

26
Q

Copper poisoning treatment

A

Penicillamine

including tx for Wilson disease

27
Q

Cyanide poisoning treatment

A

nitrite + thiosulfate

Hydroxycobalamin

28
Q

Digitalis overdose treatment

A

Anti-digoxin Fab fragments

29
Q

Iron poisoning treatment

A

Deferoxamine, deferasirox, deferiprone
(all have “fer” in their name)

Includes treatment for hemochromatosis

30
Q

Mercury poisoning treatment

A

dimercaprol

merc = mercury poisoning

31
Q

Methanol poisoning treatment

A

Fomepizole

32
Q

Ethylene glycol poisoning treatment

A

Fomepizole

33
Q

Methemoglobin poisoning treatment

A

methylene blue

34
Q

Opioid overdose treatment

A

Naloxone (mu opioid antagonist)

35
Q

Salicylate overdose treatment

A

NaHCO3 to alkalinize urine

36
Q

TCA overdose treatment

A

NaHCO3 to alkalinize urine

37
Q

Warfarin overdose treatment

A 
Vitamin K (delayed)
FFP (acute)
38
Q

Heparin overdose treatment

A

protamine sulfate

39
Q

Inhaled anesthetics and blood solubility

A
  • Less blood solubility = faster onset of action (ie Nitrous Oxide)
  • More soluble in blood = slower onset of action (ie Halothane)
40
Q

Blood-gas Partition coefficient

A

Partition coefficient= solubility

  • Higher partition coefficient = higher blood solubility = slower onset of action
  • Lower partition coefficient = lower blood solubility = faster onset of action
41
Q

MAC (Minimal alveolar concentration):

A

the percentage of anesthetic in the inspired gas mixture that renders 50% of patients unresponsive

• Inversely related to potency: high MAC equals low potency, low MAC equals high potency

42
Q

Liver damage seen with acetaminophen toxicity

A

Toxicity causes hepatocyte damage: centrilobular necrosis (Zone III)

43
Q

CYP inducer or inhibitor?: Carbamazepine

A

Inducer – dec drug effectiveness

44
Q

CYP inducer or inhibitor?: St Johns Wort

A

Inducer – dec drug effectiveness

45
Q

CYP inducer or inhibitor?: Cimetidine

A

Inhibitor – inc drug effectiveness

46
Q

CYP inducer or inhibitor?: Griseofulvin

A

Inducer – dec drug effectiveness

47
Q

CYP inducer or inhibitor?: Grapefruit juice

A

Inhibitor – inc drug effectiveness

48
Q

CYP inducer or inhibitor?: Ritonavir

A

Inhibitor – inc drug effectiveness

49
Q

Patient is exposed to radioactive iodine, what do you give them?

A

potassium idodide

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