7 Medicines and Pharmacology Flashcards by Ryan Bird

Requirements for skin absorption

Based on lipid solubility through the epidermis

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Requirements for CSF absorption

Non-ionized, lipid-soluble drugs

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Why can you not use sulfonamides in newborns?

Displaces unconugated bilirubin from albumin in newborns

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Where are tetracycline and heavy metals stored?

Bone

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0 order kinetics?

Constant amount of drug is eliminated regardless of dose

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1st order kinetics?

Drug eliminated proportional to dose

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How long does it take for a drug to reach a steady state?

5 half-lives

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Volume of distribution?

Amount of drug in the body divided by the amount of drug in plasma or blood

Drugs with high VOD have higher concentrations in extravascular compartment (i.e. fat tissue) compared to intravascular concentrations

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Bioavailability

Fraction of unchanged drug reaching the systemic circulation
IV drugs - 100%
PO drugs (less)

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ED50

Drug level at which desired effect occurs in 50% of patients

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LD50

Drug level at which death occurs in 50% of patients

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Hyperactive

Effect at an unusually low dose

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Tachyphylaxis

Tolerance after only a few doses

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Potency

Dose required for effect

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Efficacy

Ability to achieve results without untoward effect

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Phase I drug metabolism

Hepatocyte smooth endoplasmic reticulum
Demethylation, oxidation, reduction,hydrolysis reactions
Mixed function oxidases
Requires NADPH/oxygen

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Phase II drug metabolism

Hepatocyte smooth endoplasmic reticulum
Glucuronic acid and sulfates attached
Forms water-soluble metabolite - usually inactive and ready for excretion
Biliary excreted drugs may become deconjugated in intestines with reabsorption, sometimes in active form

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Inhibitors of P450

Cimetidine
Isoniazid
Ketoconazole
Erythromycin
Cipro
Flagyl
Allopurinol
Verapamil
Amiodarone
MAOIs
Disulfiram

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Inducers of P450

Cruciform vegetables
ETOH
Insecticides
Cigarette smoke
Phenobarbital (barbiturates)
Dilantin
Theophylline
Warfarin

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Polar drugs

Ionized
Water soluble
More likely to be eliminated in unaltered form

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Nonpolar drugs

Non-ionized
Fat soluble
More likely metabolized before excretion

Gout

Uric acid buildup
End product of pruine metabolism
Tx: Colchicine, Indomethacin, Allopurinol, Probenecid

Colchicine

Anti-inflammatory
Binds tubulin and inhibits migration of WBCs
For Gout

Indomethacin

NSAID
Inhibits prostaglandin synthesis (reversible cyclooxygenase inhibitor)
For Gout

Allopurinol

Xanthine oxidase inhibitor Blocks uric acid formation from xanthine For Gout

Probenecid

Increases renal secretion of uric acid | For gout

Cholestyramine

Binds bile acids in gut - forcing body to make more bile acids from cholesterol Can bind vitamin K and cause bleeding tendency For hyperlipidemia

Statins

HMG-CoA reductase inhibitors Can cause liver dysfunction, rhabdomyolysis For hyperlipidemia

Niacin

Inhibits cholesterol synthesis Can cause flushing (Treat with ASA) For hyperlipidemia

Promethazine (Phenergan)

Antiemetic Inhibits dopamine receptors AE: Tardive dyskinesia (treat with benadryl)

Metoclopramide (Reglan)

Prokinetic Inhibits dopamine receptors Can be used to increase gastric and gut motility

Ondansetron (Zofran)

Antiemetic | Central-acting serotonic receptor inhibitor

Omeprazole

Anti-acid Proton pump inhibitor Blocks H/K ATPase in stomach parietal cells

Ocretotide

Long-acting somatostatin analogue | Decreases gut secretions

Digoxin

Inhibits Na/K ATPase - increasing myocardial calcium Slows atrial-ventricular conduction, ionotrope AE: Decreases blood flow to intestines - mesenteric ischemia; Hypokalemia (precipitate arrhythmias/AV block); yellow hue, fatigue, arrhythmias NOT cleared by dialysis

Amiodarone

Good for acute atrial and ventricular arrhythmias | AE: pulmonary fibrosis with prolonged use, hypo/hyperthyroidism

Magnesium

Used to treat torasdes de pointes (ventricular tachycardia)

Adenosine

Causes transient interruption of the AV node

ACE inhibitors

Can prevent CHF after MI Can prevent progression of renal dysfunction in HTN, DM Can precipitate renal failure in renal artery stenosis

Best single agent to improve survival in patients with CHF

ACE inhibitors

Beta-blockers

Improve survival in severe LV failure | Reduces risk of MI and afib postoperative

Best single agent to improve survival in patients after MI

Beta-blockers

Atropine

Acetylcholine antagonist | Increases heart rate

Metyrapone | Aminoglutethimide

Inhibits adrenal steroid synthesis | Used in patients with adrenocortical CA

Leuprolide

Analogue of GnRH and LHRH Inhibits release of LH and FSH from pituitary when given continuously Used in patients with metastatic prostate cancer

NSAIDs

Inhibit prostaglandin synthesis and leads to decrease in mucus and HCO secretion and increased acid production

Misoprostol

PGE1 derivative Protective prostaglandin Consider use in patients on chronic NSAIDs

Haldol

``` Antipsychotic Inhibits dopamine receptors Extrapyramidal cells (treat with benadryl) ```

ASA poisoning

``` Symptoms: Tinnitus, headaches, nausea, vomiting 1st - respiratory alkalosis 2nd - metabolic acidosis Treatment - supportive ```

Most common adverse effect of gadolinium

Nausea

Most common side effects of iodine contrast

Nausea | requiring medical treatment - dyspnea

Treatment of tylenol overdose?

N-acetylcysteine