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Pharmacology > 2) Pharmacotherapeutics > Flashcards

2) Pharmacotherapeutics Flashcards

1
Q

Volume of distribution (Vd)

A
  • Volume of body fluid into which a drug is dissolved or distributed
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2
Q

The most common site for drugs metabolism

A
  • Liver

- A detoxifying machine via chemical reactions of CYP450

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3
Q

Cytochrome P450 (CYP)

A
  • Important group of enzymes responsible for a variety of Phase I reactions (1st step reactions of metabolism that biotransforms drugs, typically to MORE POLAR compounds)
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4
Q

Superfamily of CYP enzymes was classified into

subgroups using the following system

A
  • Family (40% homology, number after CYP)
  • Subfamily (60% homology, letter after CYP#)
  • Genetic isoform/variant (number following CYP#X)
  • Alleles (*# at the end)
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5
Q

Factors modifying drug actions

A
  • Physiochemical
  • Physiological
  • Pathological
  • Genetic
  • Environmental
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6
Q

Age influence on drug actions

A
  • Newborn babies & elderly are greater & more prolonged effect
  • Less efficient drug metabolism & renal functions
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7
Q

Gender influence on drug actions

A
  • Dose and response can differ between men & women
  • Metabolism of some drugs less in women (more adipose tissues)
  • Females may require doses that are on the lower side of the range
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8
Q

Pregnancy effects on drug actions

A
  • Avoid certain drugs due to teratogenic effects
  • Lipophilic drugs cross placental barrier
  • Altered body physiology during pregnancy
  • Increased cardiac output, GFR & renal elimination, volume of distribution
  • Altered metabolism of certain drugs
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9
Q

Body weight and surface area effects on drug actions

A
  • Concentration of drug at site of action = ratio of body wt. & amount of drug
  • Quantity of drug for lighter vs heavier and smaller vs larger persons
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10
Q

Diarrhea increases the motility of the gut and can

A
  • Decrease drug absorption
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11
Q

Liver disease leads to

A
  • Decreased metabolism of drug and accumulation
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12
Q

Impaired renal function leads to

A
  • Decreased drug excretion

- Drug accumulation

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13
Q

Cigarette smokers metabolize _____ more rapidly than non-smokers

A
  • Olanzapine
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14
Q

Genetic polymorphism

A
  • The variation/difference in genetic makeup

- Can affect patient response to a specific drug

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15
Q

Some drugs have a genetic testing requirement prior to use in order to avoid

A
  • Inducing a fatal ADR
  • Having no/low therapeutic effect
  • Causing significant Drug-Drug Interactions (DDIs)
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16
Q

Poor Metabolizers (PM)

A
  • Have two non-functional alleles

- Little to no enzyme activity

17
Q

Intermediate Metabolizers (IM)

A
  • Have one non-functional allele and one normally functioning allele
  • Decreased enzyme activity
18
Q

Extensive Metabolizers (EM)

A
  • Have 2 normally functioning alleles

- Normal enzyme activity

19
Q

Ultra-Rapid Metabolizers (UM)

A
  • Have one or more alleles with a mutation type

- Increased enzyme activity compared to extensive metabolizers

20
Q

CYP2B6 metabolizes 2 anti-HIV drugs

A
  • Efavirenz

- Nevirapine

21
Q

For drugs to exert a pharmacological actions, they have to

A
  • Reach the systemic circulation
  • Be in active form
  • Be free (non-complexed)
22
Q

If drugs are metabolized “prior to” reaching the circulation, they are said to

A
  • Have gone through “first pass effect” or “pre-systemic” metabolism
23
Q

Oral drugs may be exposed to first pass effect in

A
  • Extra hepatic (outside the liver)

- Hepatic

24
Q

Extra-hepatic first pass metabolism sites

A
  • P-glycoprotein system (protein of the cell membrane that pumps many foreign substances out of cells)
  • Intestinal metabolism
  • Intestinal microflora
25
Q

P-GlycoProteins (P-gp)

A
  • Efflux (E for Exit, expulsion, pumping to outside) plasma membrane protein
26
Q

P-GlycoProteins (P-gp) are implicated in many

A
  • DDIs (Drug-Drug Interactions) since many CYP3A4 substrates are also P-gp substrates
27
Q

In the gut, P-glycoprotein

A
  • Pumps drugs back into the lumen

- Decreasing their absorption

28
Q

Drugs which induce P-glycoprotein, such as rifampicin, can

A
  • Reduce the bioavailability of some other drugs
29
Q

Inhibitors of P-glycoprotein, such as verapamil,

A
  • Increase the bioavailability of susceptible drugs
30
Q

Intestinal mucosa is rich in

A
  • CYP3A4 system
31
Q

Many drugs like _____ and _____ can be affected if the gut

flora balance is disrupted

A
  • Digoxin

- Estrogens oral contraceptives

32
Q

Drugs secreted by the liver into bile are capable of undergoing

A
  • Enterohepatic recycling
33
Q

Enterohepatic recycling

A
  • The circulation of biliary acids, bilirubin, drugs or other substances from the liver to the bile
  • Followed by entry into the small intestine
  • Transported back to the liver
34
Q

Routes of administration available

A
  • Intramuscular
  • Subcutaneous
  • Intravenous
  • Intradermal
  • Transdermal
  • Sublingual
  • Oral
  • Rectal
  • Parenteral
  • Topical

Pharmacology (27 decks)

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