Chapter 7: Medicines and Pharmacology Flashcards
Drug admin: do not pass through liver first (no first-pass metabolism)
Sublingual and rectal drugs
Drug admin: Skin absorption is based on…
lipid solubility through the epidermis
Drug admin: properties for CSF absorption
nonionized, lipid-soluble drugs
Largely responsible for binding drugs (PCNs and warfarin 90% bound)
Albumin
Why are sulfonamides not used in newborns?
Sulfonamides displace unconjugated bilirubin from albumin in newborns
Where are tetracycline and heavy metals stored?
bone
Constant amount of drug is eliminated regardless of dose
Zero order kinetics
Drug eliminated proportional to dose
First order kinetics
How many half-lives for a drug to reach steady state?
5
Volume of distribution
Amount of drug in the body divided by the amount of drug in plasma or blood.
Drugs with a high volume of distribution: extravascular vs intravascular concentrations
High volume of distribution: higher concentrations in extravascular compartment (e.g., fat) compared with intravascular concentrations
Fraction of unchanged drug reaching the systemic circulation
Bioavailability
Drug level at which desired effect occurs in 50% of patients
ED-50
Drug level at which death occurs in 50% of patients
LD-50
Dose required for effect
Potency
Ability to achieve result without untoward effect
Efficacy
Drug metabolism: components of Phase 1
Demethylation, oxidation, reduction, hydrolysis reactions (mixed function oxidases, requires NADPH/oxygen)
Drug metabolism: components of Phase 2
Glucuronic acid (#1) and sulfates attached (forms water-soluble metabolite); usually inactive and ready for excretion.
Entero-hepatic recirculation (eg, cyclosporine)
biliary excreted drugs may become deconjugated in intestines with reabsorption, some in active form
Inhibitors of p-450
Cimetidine. Isoniazid. Ketoconazole. Erythromycin. Cipro. Flagyl. Allopurinol. Verapamil. Amiodarone. MAOIs. Disfulfiram.
Inducers of p-450
Cruciform vegetables. ETOH. Insecticides. Cigarette smoke. Phenobarbital (barbiturates). Dilantin. Theophylline. Warfarin.
Polar drugs
- Ionized
- Water soluble
- More likely to be eliminated in unaltered form