Week 1 & 2...

Question 1

What is the most common mode of absorption of drugs into the blood?

Answer 1

Passive transport

Question 2

Where is the best area for Acidic drugs to be absorbed?

Answer 2

In Stomach, Alkaline get processed by SI/Duodenum

Question 3

How is Acidic drug poisoning treated?

Answer 3

Sodium Bicarbonate alkaline injection

Question 4

What are the physical factors on which drug absorption depends?

Answer 4

Presence of food in ST; Blood flow - more flow =’s more absorption; Total surface area available - more surface =’s more absorption; Contact time - quick mmnt thru GI track =’s less absorption

Question 5

Solubility of a drug is best absorbed when largely ________ with some _________ ________

Answer 5

Largely Hydrophobic (fat-soluble) with some aqueous solubility (Hydrophilic)

Question 6

What is bioavailability?

Answer 6

Fraction of administered drug that reaches systemic circulation UNCHANGED —- AUC oral to AUC injected IV x 100

Question 7

Can drugs like Insulin & Penicillin be given orally? Why or Why Not?

Answer 7

No, because it will get destroyed by ST’s acidity and enzymes

Question 8

Plasma - Protein binding, is it active or inactive?

Answer 8

Free portion is active;
Bound drugs = inactive
Unbound drugs = active

Question 9

What % of body mass is fluid volume? Total body water by water weight? What is the distribution?

Answer 9

70% by body mass
60% of body weight
Plasma = 4L; Interstitial fluid = 10L; Intracellular = 28 L
Total is 42 L’s

Question 10

When drug is first absorbed it goes to _______ 1st.

Answer 10

Plasma - up to 4L’s then to Interstitial fluid (up to 10L), then into intracellular. Drugs like Heparin don’t make it past plasma, but Alcohol goes to entire body.

Question 11

_________ is the time taken to reduce drugs concentration in plasma by 1/2. What is the level called at it’s lowest peak? Highest peak?

Answer 11

Half-life; lowest peak = trough level & highest = peak level
Ex: 9am concentration = 300 mg/L
3PM concentration = 150 mg/L
9PM concentration = 75mg/L

*Will change with a patients body condition - need to monitor

Question 12

Which class of drug is mostly bound with a bit loose in the plasma?

Answer 12

Class 1 - smaller dose drugs - goes directly to plasma (4L) and bound mostly with plasma.

Question 13

Which class of drug are high dosed and saturated with a lot ending up loose in the plasma?

Answer 13

Class 2 - Sulfonamide/Antibiotic) - larger dose drugs - saturated so more unbound agents.

Question 14

Which drugs need to be monitored on a regular basis?

Answer 14

Dangerous drugs - Cumadine; Dimatine - Seizures/Epilepsy

• If LV does not Fx well concentration will go high bc metabolizes and excretes.

Question 15

What is Volume of distribution? Which type of drug will have larger distribution?

Answer 15

• The range of which the drug has been distributed across a larger volume of fluid in the body. Dose/Plasma of concentration = Volume of distribution.
• Drug with larger half life will have larger distribution. - Drugs with smaller half-life will be distributed only in plasma (4L)

Question 16

Drugs mostly bind with _______

Answer 16

Albumins

Question 17

Heparin is mostly distributed in _______.
Aminoglycosides are mostly distributed in plasma & _______ _______.
And Ethanol is distributed in ______ _____.

Answer 17

Heparin = Plasma
Aminglycosides = plasma & interstitial fluid
Ethanol = into total body water

Question 18

Tolbutamide is a Class ______ drug

Answer 18

Class 1 - smaller dose

Question 19

Sulfonamide Antibiotic is a Class ____ drug

Answer 19

Class 2 - large dose - 500+

Question 20

Phase ____ reactions - drugs are oxidized or reduced to a more polar from. Most of the phase ____ reactions utilize the Cytochrome P450 system of enzymes. (in SER- esp in LV)

Answer 20

Phase 1; phase 1 = Cytochrome P450 enzymes - oxidation & reaction allowing for excretion synthesis to happen. Example - Ethanol increases synthesis of cP450 enzymes which metabolize it making patient more immune over shorter time.

Question 21

Phase ______ reactions - a polar group such as glutathione is conjugated to the drug substantially increasing the polarity of drug. highly polar drugs can be excreted to KD.

Answer 21

Phase 2 - causes conjugation reaction or excretion

Question 22

A sympathetic drug receptor _______ heart rate. And a parasympathetic drug receptor ________ heart rate.

Answer 22

Sympathetic/ADRENERGIC = Increases HR (Dilate bronchioles) - fluids decrease - activated by epinephrine & norepinephrine

Parasympathetic/CHOLINERGIC - lowers HR (Constricts Bronchioles) - fluids increase - activated by Acetylcholine

Both work to stimulate or block receptors of ANS under PNS

Question 23

Metabolism of drugs mostly happens in _______

Answer 23

LV

Question 24

Rifampin, Phenobarbital, Carbamazepine are common enzyme __________

Answer 24

Inducers

Question 25

Erythromycin, Omeprazole, Ritonavir are common enzyme ________

Answer 25

Inhibitors

Question 26

Drugs are eliminated via _______, ________, _______ & _______

Answer 26

urine (KD) - most important route, sweat (lungs), lactation (breasts) & feces (bile/intestines)

Question 27

Ligand-gated (GABA), G-protein couple (a/b adrenoceptors), Enzyme linked (Insulin) & Intracellular (steroid) are 4 types of __________

Answer 27

Receptors

Question 28

________ = any drug which alters physiology of a cell - produces action

Answer 28

Agonist (Strong Agonist - maximal effect & weak agonist must be bound to many more receptors and produces partial action)

Question 29

____________ = inhibits or blocks responses of drugs

Answer 29

Antagonist

Question 30

__________ is the degree to which a drug is able to induce maximal effects

Answer 30

Efficacy

Question 31

_________ is the amount of drug required to produce 50% of the maximal response that the drug is capable of inducing.

Answer 31

Potency