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Drug definition

Any substance acting on a biological system that can bring about a change in biological function through its chemical actions.

1

PharmacoDynamics?

Actions of drug on the body.
PharmacoDynamics: Drug --> body

2

PharmacoKinetics?

Actions of the body on the drug.
PharmacoKinetics: Katawan --> drugs

3

Lightest drug in terms of molecular weight?

Lithium. MW 7 .
Used for bipolar disorders.
WOF nephrogenic diabetes insipidus

4

Heaviest drug?

Alteplase. MW 50,000.
Thrombolytic.

5

Anticoagulant of choice in pregnancy?

Heparin. It cannot cross the placenta because of its large size.
Vs warfarin that can cross placenta baby bleeds.

6

Heparin?

A hepe named PiTT with a large belly.
Heparin is large. i: intrinsic factor
MOA: increases antithrombin III. Monitored with PTT.
Antidote: protamine sulfate

7

Strongest bond

Covalent > ionic > hydrophobic

8

Organophosphate poisoning?

Cholinergic toxicity. DUMBELLS
Diarrhea, Urination, Miosis, Bronchocospasm,
Emesis, Lacrimation, Lethargy, Salivation

9

Antidote to organophosphate poisoning?

Pralidoxime but only for the first 6-8 hours. After that covalent bonds can no longer be broken by it.
Atropine may also be used.

10

Permeation?

Movement of drug molecules into and within biological environments.

11

Components of pharmocoKinetics?

ADME
Absorption, Distribution, Metabolism, Elimination

12

Vitamin B12 is bound to?

Intrinsic factor

13

Iron is bound to?

Transferrin for transport
Ferritin for storage

14

Fick's law of diffusion?

Absorption is faster through thinner membranes and in areas with larger surface area.

15

Henderson hasselbalch dissociation of weak acids

Protonated acid more lipid soluble, crosses biological membranes easier, unprotonated acid more water soluble, better clearance.

16

Henderson hasselbalch dissociation of weak bases

Unprotonated base more lipid soluble, better at crossing biological membranes.
Protonated base more water soluble, better clearance

17

Excretion of a weak acid may be accelerated by?

Alkalinizing urine with bicarbonate

18

Excretion of weak base accelerated by?

Acidifying urine with ammonium chloride.

19

First pass effect?

Drug is metabolized in the gut wall, the liver, and the portal circulation before it reaches the bloodstream.

20

Which quadrant of the buttocks is safest for IM drug administration?

Superolateral is safest.
Inferomedial WOF sciatic nerve

21

Sublingual route:

Lingual vein --> IJV --> brachiocephalic (innominate) vein --> SVC --> RA

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Rectal route with first pass

If superior rectal vein from IMV --> portal vein, thus first pass

23

Topical preparations:

Acute inflammation --> drying agents
Chronic inflammation --> lubricating agents

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Absorption

Transfer from site of administration to blood stream

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Distribution

Leaves blood stream to enter target organ

26

Drug binding

Acidic drugs --> albumin
Basic drugs --> orosomucoid

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Termination of drug action

Excretion

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Release of drug and metabolites through urine, stool etc

Excretion

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Rate of elimination is proportionate to concentration. Decrease by 50% for every half life decrease. Exponential decrease. Most common type

First-order elimination

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Rate of elimination is constant regardless of concentration. Decrease is linearly.

Zero order elimination

31

Drugs that follow zero order kinetics

WHAT PET
Warfarin, Heparin, Aspirin, Tolbutamide, Phenytoin
Ethanol, Theophylline

32

Kd, EC50, Emax

Kd concentration required to bind half of the receptors
Emax efficacy
EC50 potency

33

ED50, TD50, LD50

ED50 median effective dose
TD50 median toxic dose
LD50 median lethal dose

34

Maximal effect an agonist can produce if the dose is taken to very high levels

Efficacy

35

Amount of drug needed to produce a given effect.
Graded dose dose required to produce 50% of the maximal effect.
Quantal dose response ed50 ld50 td50

Potency

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Capable of fully activating the receptor system when bound.
High concentrations result in all receptors being activated

Full agonist

37

Produces less than the full effect even when the agonist has saturated all of the receptors.
Acts as an inhibitor when mixed with full agonist.

Partial agonist

38

Blocks or dampens drug response in the presence of an agonist

Antagonist

39

Binds reversibly, does not activate the effector system.
Shifts curve to the right. Increases ed50 decreased potency.
Can be overcome by adding more agonist

Competitive or reversible antagonist

40

Causes downward shift if the curve. Decreased efficacy Emax, same potency.
Not overcome by adding more agonist

Non-competitive or irreversible antagonist

41

Binds to a different receptor
Produces an effect opposite to that produced by the drug it is antagonizing.

Physiologic antagonist

42

Interacts directly with the drug being antagonized to remove it or to prevent it from binding

Chemical antagonist

43

Terazosin vs. norepinephrine
Beta blockers

Competitive or reversible antagonist

44

Phenoxybenzamine for pheochromocytoma

Non competitive irreversible antagonist

45

Histamine and epinephrine
Propranolol and thyroid hormone

Physiologic antagonist

46

Dimercaprol for heavy metal/lead poisoning
Pralidoxime for organophosphate poisoning

Chemical antagonist

47

Tachyphylaxis responsiveness diminishes, frequent exposure results in short-term dimunition

MED Loves CNN in HD
Metoclopromide, Ephedrine, Dobutamine, LSD,
Calcitonin, Nitroglycerin, Nicotine, Hydralazine, Desmopressin

48

Reversed by depletion of missing substrates

Tolerance

49

Idiosyncratic drug responses

Chloramphenicol and aplastic anemia
Allopurinol and cataracts

50

Drug eliminated with first-order kinetics, clearance is constant

Ratio
Elimination is proportional to concentration

51

Drugs eliminated with zero order kinetics clearance is constant

Amount.

52

Bioavailability is fraction of administered dose reaching systemic circulation.

It is determined by computing the area under the plasma concentration curve.

53

Maintenance dose computation

The Vd or volume of distribution is not in voiced in calculating for maintenance dose

54

Loading dose computation

Does not include clearance

55

Phase 1 reactions convert the parent drug to a more water-soluble polar product.examples are

HORD of phase 1
Hydrolysis, Oxidation, Reduction, Deamination

56

75% of drugs are metabolized by

CYP3A4 and CYP2D6

57

Enzyme induction

Increased synthesis of cyp450 enzymes and heme. Higher amount of the drug needed due to increased metabolism, excretion.

58

Enzyme inducers

ETHYL Booba takes PHEN and RIFuses GRISy CARB Shakes
Ethanol, Barbiturates, PHENytoin, RIFampicin, GRISeofulvin, St. John's Wort/Smoking

59

Most potent enzyme inducers

Carbamazepine phenobarbital phenytoin RIFampicin

60

Enzyme inhibition

Lower doses of a drug are needed, drug stays in the system longer, reduction in blood flow to metabolizing organ

61

Suicide inhibitor

Metabolized to products that irreversibly inhibit the metabolizing enzyme.

62

Suicide inhibitors

Ethinyl estradiol, spirinolactone, allopurinol, PTU

63

Enzyme inhibitors

Inhibitors Stop CIber KEds from Eating GRApefruit Q
Isoniazid, Sulfonamide, Cimitedine, Ketoconazole, Erythromycin, Grapefruit juice, Ritonavir, Amiodarone, Quinidine

64

Category A

Human studies display no risk to fetus.

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Animal studies do not show risk, but no human studies have been conducted. Or risk in animal studies but none displayed in human studies

Category B

66

Category C

Animal studies have shown adverse effects, no human studies done. Potential benefit justifies risk to fetus

67

Category D

Evidence if human fetal risk, but potential benefits justifies risks

68

Category x

Fetal adverse effects demonstrated, risk of fetal effects outweighs any benefit of drug. Absolute contraindications.

69

DES

Vaginal clear cell adenoCA

70

Misoprostol as teratogenic

Möbius sequence

71

Thalidomide

Phocomelia

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Tetracycline

Tooth discoloration

73

Lithium

Atrialization of right ventricle. Ebstein's anomaly.

74

Standard in vitro test for mutagenicity

Ames test

75

Carcinogens

Coal tar, aflatoxin, nitrosamines, urethane, vinyl chloride, polycyclic aromatic hydrocarbons in cigarette