Pharmacology Flashcards

1
Q

Acidic drugs, such as phenytoin, bind primary to which one of the following plasma proteins?

A. Alpha-fetoprotein (AFP)
B. Lipoprotein
C. Albumin
D. Alpha-acid gylcoprotein (AAG)
E. Gamma globulin

A

Albumin

The main drug-binding proteins in plasma are albumin, apha1-acid glycoprotein and lipoproteins.

Albumin binds drugs and ligands, reducing serum concentration of these compounds. An example is serum calcium, the free (ionised) fraction needs to be corrected for albumin.

Drugs that are important for albumin binding are warfarin, digoxin, NSAIDs and benzodiazepines

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2
Q

What is the mechanism of action of clopidogrel?

A

Selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation

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3
Q

RANKL is the target for which DMARD?

A

Denosumab
- Binding RANKL suppresses bone resorption and slows progression of bone erosions

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4
Q

Medications to avoid with tamoxifen?

A

Bupropion, fluoxetine - strong CYP2D6 inhibitors
- Thus decrease tamoxifen activation

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5
Q

Isosorbide mononitrate MOA

A

Improves myocardial O2 delivery via coronary vasodilation and ↓ O2 demand via ↓ preload > ↓ ventricular wall stress

Needs nitrate-free interval 8-12 hrs to reduce tolerance

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6
Q

MOA sotolol

A

K channel blocker; may prolong QT interval

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7
Q

What does high hepatic extraction ratio mean?

A

High enzyme activity metabolising the drug - thus almost all drug is removed

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8
Q

Does loading dose influence time taken to reach steady state?

A

NO
- It brings the mean concentration of drug to higher concentration, meaning reaches therapeutic range sooner BUT does not influence time to SS

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9
Q

MOA of ciclosporin?

A

IL2 antagonist

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10
Q

Tacrolimus MOA?

A

IL2 antagonist; better immunosuppression but more nephrotoxic and worse BGL control
- Tacrolimus inhibits T-lymphocyte activationby binding to FKBP-12, an intracellular protein

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11
Q

Indication for dialysis in chronic lithium toxicity?

A

Lithium level >2.5 and CNS involvement

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12
Q

What does the BCG vaccine protect against?

A

BCG vaccine has a documented protective effect against meningitis and disseminated TB in children. It does not prevent primary infection and, more importantly, does not prevent reactivation of latent pulmonary infection, the principal source of bacillary spread in the community

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13
Q

Rifampicin inducer or inhibitor?

A

RifampicINDUCER

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14
Q

MOA metaclopramide?

A

D2 antagonist
- CTZ in medulla oblongata

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15
Q

Medications which cause B12 deficiency

A

Alcohol, metformin, PPI, colchicine, phenytoin

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16
Q

Phenytoin SE

A

CYP inducer

B12 + folate deficiency
Gum hypertrophy
Hypotension
Purple glove syndrome (limb oedema and discolouration from crystallisation in blood)

17
Q

Lamotrigine + sodium valproate interaction?

A

Valproate competitively inhibits lamotrigine metabolism > increased levels of lamotrigine

Large Lamotrigine

18
Q

Which medication used in EtOH addiction are contraindicated in heart disease?

A

Disulfuram

19
Q

Lamotrigine + carbemazepine?

A

Decrease in lamotrigine levels
- Carbemazepine is an inducer

Crap lamotrigine; crap levels (low)

20
Q

Palliative care dosing

A

β€’ Morphine PO to SC = 2:1
β€’ PRN dosing = 1/6 TDD
β€’ Morphine to hydromorphone = 5:1
β€’ Morphine to fentanyl: 1:100

21
Q

Fenofibrate MOA?

A

Lower lipid levels by activating PPARΞ± > increase lipolysis and elimination of triglyceride-rich particles from plasma

22
Q

Hysteresis loop characteristics?

A

Tachyphylaxis
- Tolerance develops rapidly, but effect and concentration decreases overtime
- Amphetamines, cocaine

23
Q

Reverse hysteresis loop characteristics?

A

Lag time of medication
- MORE effect over time
- Occurs in: prodrug/active metabolites, secondary messengers, redistribution

24
Q

Features of cholinergic crisis

A

SLUDGE

S: Salivation
L: Lacrimation
U: Urination
D: Diaphoresis
G: Gastrointestinal upset
E: Emesis

25
Q

Serotonin syndrome vs. neuroleptic malignant syndrome

A
26
Q

Probenecid MOA?

A

Inhibition of organic anionics transporter, reducing excretion

27
Q

Interaction between sodium valproate and carbapenems (meropenem, ertapenem, imipenem)?

A

Decreased efficacy of sodium valproate

28
Q

Which antibiotics are bacteriocidal

A

Bactericidal
* Aminoglycosides: Tobramycin, gentamicin, amikacin
* Beta-lactams (penicillins, cephalosporins, carbapenems): Amoxicillin, cefazolin, meropenem
* Fluoroquinolones: Ciprofloxacin, levofloxacin, moxifloxacin
* Glycopeptides: Vancomycin
* Cyclic Lipopeptides: Daptomycin
* Nitroimidazoles: Metronidazole

29
Q
A
30
Q

COX summary

A