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Basic Principles Flashcards

0
Q

Actions of body on drug

A

Pharmacokinetics

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1
Q

Actions of drug on body

A

Pharmacodynamics

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2
Q

Passive movement of non protein bound drugs between blood and extravascular space through small water filled pores
Affected by DRUG CONCENTRATION and CHARGE

A

Aqueous diffusion
Permeation
Pharmacokinetics

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3
Q

Exceptions to aqueous diffusion

A

Brain
Testes
Eye
Placenta

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4
Q

Most important limiting factor for permeation in the BBB and placenta

A

CONCENTRATION
Lipid Diffusion
Pharmacokinetics

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5
Q

Transport NOT GOVERNED BY FICK’s LAW is limited by

A

CAPACITY
Transport by special carriers
Pharmacokinetics

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6
Q

Endocytosis is limited by

A

CAPACITY

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7
Q

Fick’s Law of Diffusion

A

C1-C2 x surface area x (permeability coefficient/thickness)

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8
Q

Implications of Fick’s Law

Absorption is faster in

A

LARGER SA SI>stomach

THINNER MEMBRANES lungs>skin

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9
Q

Partial avoidance of first pass effect

A

Rectal
SRV: IMV to PV
MRV: IIV to IVC
IRV: IPV to IIV to IVC

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10
Q

Slowest route of administration

A

Topical

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11
Q

More evaporation

Less evaporation

A

Tinctures

Ointments

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12
Q

Acidic drugs are bound to

Basic drugs are bound to

A

Albumin

Orosomucoid

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13
Q

Reversible
Shift to R - inc potency - add more S
Examples

A

Competitive antagonist

Propanolol B blocker and Isoproterenol B agonist

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14
Q

Irreversible
Downward shift - Emax lowered
Examples?

A

Norepinephrine and phenoxybenzamine

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15
Q

Binds to a different receptor causing the opposite effect

Examples?

A

Physiologic antagonists

Histamine and epinephrine

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16
Q

Propanolol and thyroid hormone

A

Inverse agonist
Reduces constitutive activity
Binds with the same receptor to produce opposite effect

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17
Q

Interacts directly with drug

A

Chemical antagonists
Dimercaprol for lead poisoning
Pralidoxime for organophosphate poisoning

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18
Q

Tachyphylactic drugs

A 
MED students Love to watch CNN in HD
Metoclopramide
Ephedrine
Dobutamine
LSD
Calcitonin
Nitroglycerin
Nicotine
Hydralazine
Desmopressin
19
Q

Tolerance examples

A

Depletion of thiol cofactors in nitroglycerin

- glutathione

20
Q

Idiosyncratic drug response

A

Aplastic anemia / chloramphenicol

Cataracts / allopurinol

21
Q

Vd
Blood
ECF
Tissue

A

Low
Med
High

22
Q

Amount Vd

A

Amount of drug in body / plasma drug concentration

Liver and kidney dependent

23
Q

Clearance

A

Rate of drug elimination / plasma drug concentration

24
Q

Steady state

A

4-5 half lives

25
Q

Half life

A

0.693 x vd / cl

26
Q

Maintenance dose

A

Cl x desired plasma concentration / bioavailability

Vd is NOT involved

27
Q

Cl is NOT involved

A

Loading dose

28
Q

Corrected dose

Renal disease or reduced cardiac output

A

Average dose x (Clcr / 100ml/min)

29
Q

Clcr

A

(Wt x (140-age)) / (72 x serum crea)

x 0.85 in females

30
Q

Phase 1 reactions

CYP3A4 and CYP2D6

A 
More water soluble
HORDe
Hydrolysis
Oxidation
Reduction
Deamination
31
Q

Phase 2 reactions

A

Conjugation to polar groups

32
Q

CP450 Inducers

A 
Ethyl Booba takes Phen-Phen and Refuses Greasy Carb Shakes
Ethanol
Barbidurates
Phenytoin
Rifampin
Griseofulvin
Carbamazepine
St. John's Wort/Smoking
33
Q

CP450 Inhibitors

A 
Inhibitors Stop Cyberkids from Eating Grapefruit QV
Isoniazid
Sulfonamides
Cimetidine
Erythromycin
Grapefruit
Quinidine
Valproic acid
34
Q

Administration of single doses of the agent up to the lethal level in at least 2 species

A

Acute toxicity

Animal testing

35
Q

Animal testing
Acute toxicity
Subacute and chronic testing

A

Pharmacologic profile

36
Q

Reproductive toxicity

A

Teratogenesis devt defects
Mutagenesis heritable
Carcinogenesis malignancy

37
Q

A
Pregnant Animal Studies
Pregnant Human Studies

A

Safe
Safe
Folic acid and thyroid hormones

38
Q

B
Pregnant Animal Studies
Pregnant Human Studies

A

Safe
None

Unsafe
Safe

Zidovudine

39
Q

C
Pregnant Animal Studies
Pregnant Human Studies

A

Unsafe
None

None
None

Aspirin

40
Q

D
Pregnant Animal Studies
Pregnant Human Studies

A

Unsafe
Unsafe

ACE inhibitors
Anti convulsants

41
Q

X
Pregnant Animal Studies
Pregnant Human Studies

A

Unsafe
Unsafe

Statins, OCP, Clomiphene, Misoprostol, High dose Vit A

42
Q

Teratogens

ACE inhibitors

A

Fetal renal damage

43
Q

In vitro test for mutagenicity

44
Q

In vivo test for mutagenicity

A

Dominant lethal test

45
Q 
Clinical trials
Phase 1
Phase 2
Phase 3
Phase 4
A

Is it safe? Normal volunteers Except cancer and toxic agents
Is it effective? Sick volunteers
Is it better?
Postmarketing

46
Q

Bioequivalent

A

Comparable bioavailability

Similar times to achieve peak blood concentrations

Pharmacology (33 decks)

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