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12 Cards in this Set

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What are pharmacokinetics?

Pertains to the collection of processes involved in drug disposition



What the body does to a drug



Thus determining the concentration of drug delivered to the target effector molecules



Includes absorption, distribution, metabolism, and excretion [ADME]

What are pharmacodynamics?

Pertains to the effects of the drug



What the drug does to the body and the mechanisms of actions of that drug



The effect of any drug depends predominantly on the presence, abundance, and characteristics (pharmacogenetics) of the specific molecular receptor

How can pregnancy affect the absorption of a drug?

Intestinal motility: M > F > pregnant F



Gastric pH: acidity M > F > preg F (pregnancy decreases absorption of weak acid)



Gastric emptying: M > F > preg F



Dermal hydration is increased in pregnant F (altered absorption of topical agents)



Body surface area: M > pregnant F > F



Skin blood flow: increased in pregnant F (absorption increased)



Pulmonary function: M > pregnant F > F



Cardiac output: M > pregnant F > F

How does pregnancy affect the distribution of a drug?

Plasma volume: pregnant F > M > F (decreased concentration in pregnancy)



Average organ blood flow: pregnant F > M > F



Total body water: M > pregnant F > F



Plasma proteins: M, F > pregnant F



Body fat: pregnant F > F > M



Cardiac output: M > pregnant F > F

What happens during the two phases of drug metabolism? What type of enzymes are involved in each phase? How can sex affect these phases?

Phase 1 (oxygenases) → mostly through CYP3A


- loss of electrons or an increase in oxidation state by a molecule



Phase 2 (transferases)


-addition of a molecule to the drug that changes activity or disposal



Each enzyme has specific inhibitors and inducers



Specific sex differences that can be increased or reduced because of these inhibitors and inducers



Sex differences is most phase 1 enzymes (males usually have greater activity than females, except CYP3 where females may have more activity than males)

How does elimination of a drug differ in men and women?

Drugs that are excreted in the urine are cleared more slowly in women (lower cardiac output → lower renal blood flow)



Medications with decreased renal clearance in women: Digoxin, methotrexate, aminoglycosides, cephalosporins, fluoroquinolones, vancomycin, anticonvulsants (gabapentin and pregabalin)



To account for variations in clearance, women should receive lower dosages of these medications based on GFR

Which sex has a higher incidence of adverse drug reactions? What could this be due to?

Females



Mass, height, body surface, fat, respiratory function, cardiac output


-tissue mass of various organs (i.e. liver, kidney, and lungs are all smaller), fat concentration is higher


-reduced blood flow rates to liver, kidney, and skeletal muscle


-all organs that participate in drug metabolism put women at a disadvantage if given the same dose as a man

What is the pharmacological reason and factors that make it common for women to be overdosed?

Pharmacokinetics



Factors:


-sex differences in volume of distribution


-sex differences in protein binding of drug


-sex differences in transport, phase 1, and phase 2 metabolism

What is the pharmacological reason and factors that make women more sensitive to many drugs?

Pharmacodynamics



Factors: sex differences in drug targets


-receptor number


-receptor binding


-signal transduction following receptor binding

What is the pharmacological reason and factors that make it common for women who are prescribed multiple medications to have adverse effects?

Drug-drug interactions



Factors: drug-drug induced alterations, pharmacokinetics, pharmacodynamics

What is an example of a pharmacokinetic drug-drug interaction?

A drug that increases the plasma concentration of another drug



A drug that inhibits the metabolism of another drug

What is an example of a pharmacodynamic drug-drug interaction?

A drug that increases the risk for a patient to develop serotonin syndrome when given with another drug