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[MT 6314] - 1st Shifting > [5] Biotrans 2.5 - 4 > Flashcards

[5] Biotrans 2.5 - 4 Flashcards

1
Q

PECULIARITY ON METABOLIZING DRUGS

Maybe metabolized by gastric fluid

Must be given 2 hours before meals if given
through the oral route

A

PENICILLIN

Lower bioavailability

Must be given 2 hours before
meals so that the gastric acids
cannot degrade it

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2
Q

PECULIARITY ON METABOLIZING DRUGS

Cannot be given in the
oral route as it will be
degraded down as amino
acids

Should be given
subcutaneously

A

Insulin

Short half life; you need to
give it 30 minutes prior to
the intake to mimic the
natural secretion of
insulin

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3
Q

PECULIARITY ON METABOLIZING DRUGS

Intestinal wall enzymes:

Especially for those who have cardiac arrests  to stimulate pumping of the heart

Given intravascular/
intravenously

A

Epinephrine

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4
Q

Most important organ for drug metabolism

Smooth endoplasmic reticulum (SER) contains high
concentration of PHASE I enzymes

A

LIVER

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5
Q

PHASE I enzymes: Activity of these enzymes require…

A

NADPH (reducing agent)
- REdox reactions
Molecular form of oxygen
- Final electron acceptor

That’s why the liver is bombarded
with many reactive oxygen species
and will try to
regenerate/neutralize them

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6
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

(3) GENETIC FACTORS:

A
  • HYDROLYSIS OF ESTERS
  • ACETYLATION OF AMINES - SLOW ACETYLATORS
  • OXIDATION
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7
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

GENETIC FACTORS: In most individuals, the process occurs rapidly. Some individuals cannot hydrolyze esters properly

A

HYDROLYSIS OF ESTERS

Duration of action is 5 minutes

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8
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

GENETIC FACTORS: Succinylcholine. Ester that is metabolized by plasma cholinesterase

Plasma cholinesterase has high metabolizing activity Trivia: plasma cholinesterase = same nzyme that degrades acetylcholine

A

HYDROLYSIS OF ESTERS

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8
Q

ACETYLATION OF AMINES - SLOW ACETYLATORS

T/F: If you are a slow acetylator, you are prone to hepatotoxicity when given such drug

A

True

Not a problem in Filipinos because we are
fast acetylators compared to other
individuals

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9
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

GENETIC FACTORS: Isoniazid (INH) - (Anti TB drug) .Amines such as hydralazine, and procaina

Individuals deficient in acetylating capacity

A

ACETYLATION OF AMINES - SLOW ACETYLATORS

○ If you have high levels of this drug in your system, it can produce toxic effects
○ Quite hepatotoxic

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10
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

GENETIC FACTORS: Dextromethorphan, metoprolol and some tricyclic
antidepressants

Some are dependent on enzyme activity present in
the body

A

OXIDATION

Oxidation by P450 isoenzymes are genetically
predetermined

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11
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

(2) INDIVIDUAL DIFFERENCES

A

Diet and environmental factors
Age and sex

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12
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

INDIVIDUAL DIFFERENCES: Grapefruit juice increases the amount of
drug in the body

Some food supplements include
grapefruit juice which would
increase the amount of drug in the
body

A

Diet and environmental factors

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12
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

INDIVIDUAL DIFFERENCES: Charcoal inhibits the effect of the drug

  • Activated charcoal used to neutralize poisoning
  • Inhibition would require a higher
    dose to achieve its effect
A

Diet and environmental factors

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13
Q

DETERMINANTS OF BIOTRANSFORMATION RATE

INDIVIDUAL DIFFERENCES: Drug metabolites differ in young and old

In the extreme of ages, the very young and very old, metabolize the drug slower than that of a normal
adult

A

● Age and sex

It is susceptible for children and
elderly to have adverse effects
because these drugs are tested on
normal adults.

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14
Q

DISEASE AFFECTING DRUG MECHANISM

hormone increases the metabolism
which increases the drug metabolism.

● Hyperthyroidism

A

Thyroid hormone

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15
Q

When a drug is tagged as an enzyme inducer, it
means that it will increase the rate of synthesis of the metabolizing enzyme that degrades the drug.
- ENZYME INDUCTION
- ENZYME INHIBITION

A
  • ENZYME INDUCTION
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16
Q

Increase rate of synthesis of the enzyme
- ENZYME INDUCTION
- ENZYME INHIBITION

A

ENZYME INDUCTION

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16
Q

Reduce the rate of degradation of the enzyme
- ENZYME INDUCTION
- ENZYME INHIBITION

○ May also induce self metabolism of the drug
○ May also induce metabolism of other drugs and reduce its effect

A
  • ENZYME INDUCTION
17
Q

○ Phenobarbital
○ Carbamazepine + drug = decreased effects
○ Phenytoin
○ Rifampicin

  • ENZYME INDUCTION
  • ENZYME INHIBITION
A
  • ENZYME INDUCTION
18
Q

Inhibit CP450
- ENZYME INDUCTION
- ENZYME INHIBITION

A
  • ENZYME INHIBITION
19
Q

Metabolism of the drug is diminished

  • ENZYME INDUCTION
  • ENZYME INHIBITION
A

ENZYME INHIBITION

20
Q

Increase effect of the drug

  • ENZYME INDUCTION
  • ENZYME INHIBITION
A
  • ENZYME INHIBITION
21
Q

Enzyme inhibitors of ENZYME INHIBITION

ACKRF

A

○ Amiodarone
○ Cimetidine
○ Ketoconazole + drug = increased effect
○ Ritonavir
○ Furanocoumarin

22
Q

4 TYPES OF DRUG INTERACTION MECHANISM

A

Altered absorption
Altered metabolism
Altered plasma binding protein
Altered excretion

23
Q

TYPES OF DRUG INTERACTION MECHANISM

Cholestyramine inhibits the effect digoxin
when combined with it

  • Altered absorption
  • Altered metabolism
  • Altered plasma binding protein
  • Altered excretion

Since they are intestinal binders,
they will decrease the absorption
of the digoxin

A

Altered absorption

24
Q

TYPES OF DRUG INTERACTION MECHANISM

Affects drug action

  • Altered absorption
  • Altered metabolism
  • Altered plasma binding protein
  • Altered excretion

Either through enzyme induction or enzyme inhibition

A

Altered metabolism

25
Q

TYPES OF DRUG INTERACTION MECHANISM

Plasma proteins combined with drugs with
high plasma protein binding, the plasma
proteins can actually diminish the amount
of drug that reaches the receptors.

  • Altered absorption
  • Altered metabolism
  • Altered plasma binding protein
  • Altered excretion

They will compete.

Whichever has the highest protein binding
will be the one to stick, thus it will increase
the concentration of the other drug

A

Plasma proteins combined with drugs with

26
Q

TYPES OF DRUG INTERACTION MECHANISM

Probenecid inhibits the secretion of weak
acids

  • Altered absorption
  • Altered metabolism
  • Altered plasma binding protein
  • Altered excretion
A

Altered excretion

27
Q

TYPES OF DRUG INTERACTION MECHANISM

Penicillin inhibits the excretion of
probenecid

  • Altered absorption
  • Altered metabolism
  • Altered plasma binding protein
  • Altered excretion
A

Altered excretion

28
Q

(4) DRUG INTERACTION

A

ADDITIVE (=)
SYNERGISTIC (>)
POTENTIATION (enhances)
ANTAGONISM (inhibits)

29
Q

DRUG INTERACTION

1 + 1 = 2

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

In an arcade, this would be a double hit

A

ADDITIVE (=)

30
Q

DRUG INTERACTION

Response elicited by combined drugs is equal to the combined response of the individual drugs

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)
A

ADDITIVE (=)

31
Q

DRUG INTERACTION

Combining drugs with similar effects would have the combined effect of the two drugs

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)
A

ADDITIVE (=)

32
Q

Sedative + alcohol

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

For example, drinking a sedative like
phenylpropanolamine with alcohol would
increase the sleepiness effect (you’ll fall
asleep faster)

A

ADDITIVE (=)

33
Q

DRUG INTERACTION

1 + 1 = 3

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

Like a combo hit of a power-up

A

SYNERGISTIC (>)

34
Q

DRUG INTERACTION

Response elicited by combined drugs is greater than the combined responses of each individual

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

Combining the two drugs would make it more effective

A

SYNERGISTIC (>)

It is not just an added effect, but synergistic

35
Q

DRUG INTERACTION

Penicillin G removes the cell wall

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

Gentamicin inhibits production of protein

Individually, each drug could kill the
bacteria, but it would take longer

A

SYNERGISTIC (>)

36
Q

0 + 1 = 2

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)
A
  • POTENTIATION (enhances)
37
Q

Drug which has no effect enhances the effect of the second drug

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)
A

POTENTIATION (enhances)

38
Q

Cimetidine + anticoagulant (enhances the
anticoagulation)

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

Cimetidine has no anticoagulant
properties, but when combined with an
anticoagulant, the enzyme inhibiting
mechanism of cimetidine will inhibit the
metabolizing enzyme for the anticoagulant,
thus increasing the anticoagulant effect

A

POTENTIATION (enhances)

39
Q

1 + 1 = 0

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

Combining the two cancels the effect of
one another

A
  • ANTAGONISM (inhibits)
40
Q

Drug inhibits the effect of another drug

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)
A

ANTAGONISM (inhibits)

41
Q

Heparin + protamine

  • ADDITIVE (=)
  • SYNERGISTIC (>)
  • POTENTIATION (enhances)
  • ANTAGONISM (inhibits)

○ Heparin is an anticoagulant,
○ Protamine is a procoagulant

A

ANTAGONISM (inhibits)

42
Q

process of creating new medicines that can treat
or prevent diseases

A

DRUG DEVELOPMENT

[MT 6314] - 1st Shifting (23 decks)

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