Section B Flashcards

1
Q

pharmacokinetics

A

effects of the body on the drug or fate of the drug in the body

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2
Q

pharmacodynamics

A

effects of the drug on the body

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3
Q

what are the various methods of administering drugs?

A

enteral, topical, parenteral

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4
Q

list 4 examples of enteral drug administration

A

oral, nasogastric, gastronomy, buccal/sublingual

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5
Q

list 4 examples of topical drug administration

A

skin, eyes/ears/nose, inhalation, rectal/vaginal

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6
Q

list 7 examples of parenteral drug administration

A

intravenous, intramuscular, subcutaneous, intradermal, intrathecal, epidural, intra-articular

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7
Q

bioavailability

A

the fraction of the drug administered that reaches the systemic circulation

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8
Q

first pass metabolism

A

orally, some of the drug is metabolized (inactivated) before entering circulation

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9
Q

enzyme induction and its clinical relevance

A

increase in drug metabolizing enzyme activity caused by a foreign compound (inducer)
- requires prolonged exposure to inducer
- causes accelerated clearance, reduced drug action and increased formation of toxic metabolites
can cause drugs to be less effective due to rapid clearance

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10
Q

enzyme inhibition and its clinical relevance

A

decrease in enzyme activity caused by a foreign compound
- requires only single dose
- causes impaired clearance and prolonged action
can cause therapeutic levels to rise to toxic levels in drugs with small therapeutic ratios due to prolonged clearance

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11
Q

half-life

A

time it takes to eliminate half of a drug from the circulation

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12
Q

affinity

A

attractive forces between the drug and the receptor (causes drug to bind to receptor)

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13
Q

efficacy

A

ability of the drug when bound to initiate change

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14
Q

potency

A

measure of the drug at which it is effective

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15
Q

specificity

A

ability of the receptor to recognize specific chemical configurations

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16
Q

agonists

A

bind to receptors, cause conformational change, result in a response

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17
Q

antagonists

A

bind to receptors, don not cause conformational change, no activation, no efficacy, blocks agonists from binding

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18
Q

partial agonists

A

bind to receptor, but do not elicit maximal response, must occupy a large number of receptors to elicit a response

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19
Q

why are elderly patients more at risk for ADRs? (8)

A
  1. multiple illness
  2. multiple medications
  3. altered homeostasis
  4. altered immunity
  5. altered pharmacokinetics
  6. altered pharmacodynamics
  7. sensitivity to sedatives
  8. compliance problems
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20
Q

why are people with liver disease more at risk for ADRs? (5)

A
  1. encephalopathy risk (sedatives/diuretics)
  2. clotting factor synthesis not normal -> bleeding
  3. low protein affects drug binding and fluid balance
  4. metabolism abnormal -> potential for toxicity
  5. shunting affects bioavailability
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21
Q

why are people with renal disease more at risk for ADRs? (5)

A
  1. failure to excrete drugs
  2. failure to excrete metabolites
  3. increased sensitivity to drugs
  4. side-effects are poorly tolerated
  5. some drugs may be ineffective
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22
Q

what are the main groups of drugs used to treat hypertension?

A

A - ACE inhibitors & angiotensin receptor blockers (under 55 and not pregnant)
B - beta blockers
C - calcium channel blockers (over 55 or african american)
D - diuretics

23
Q

what are the mechanisms and side-effects of ACE inhibitors?

A

they block formation of angiotensin II and inhibit aldosterone release and blocks breakdown of bradykinin
Cough
Angioedema
Proteinuria
Taste changes
Orthostatic hypotension
Pregnancy fetal renal failure
Rash
Increases renin and decreases angiotensin II
Lytes - hyperkalemia due to decreased aldosterone release
-drop in BP
-fatigue
-headache
-liver damage
-renal failure

24
Q

what are the mechanisms and side-effects of angiotensin receptor blockers?

A

they bind to the angiotensin receptor and block vasoconstriction
-fatigue
-hyperkalemia
-renal failure
-syncope

25
Q

what are the mechanisms and side-effects of beta blockers?

A

they lower cardiac output, heartrate and renin secretion
B1- bradycardia
- conduction
-heart failure
B2 - bronchospasm
- vasoconstriction

26
Q

what are the indications for beta blockers?

A
  • angina
  • tremour
    -dysrhymias
  • hypertension
  • myocardial infarction
  • thyrotoxicosis
    labetalol used for malignant hypertension
27
Q

what are the mechanisms and indications for calcium channel blockers?

A

they lower calcium available to contractile proteins, lower BP, lower cardiac contractility, lower vascular smooth muscle
- angina (prevention)
- dysrhythmias
- hypertension

28
Q

what are the side-effects of calcium channel blockers? (dihydropyridine and non-dihydropyridine)

A

dihydropyridine: hypertension
- headache
- oedema
- flushing
non-dihydropyridine: not first course treatment for hypertension -> used for arrythmias
- bradycardia
- heart failure

29
Q

what are the mechanisms and side-effects (8) of diuretics?

A

they inhibit sodium transport in the distal tubule and have a vasodilator effect
e.g thiazide like drugs such as xipamide
- hypercalcemia
- hyperglycemia
- hyperuricemia
- hypochloremia
- hypokalemia
- hypomagnesemia
- hyponatremia
- blood disorders

30
Q

what do loop diuretics do? give an example and what are the side-effects?

A

inhibit sodium and potassium transport in the loop of Henley, side-effects same as diuretics e.g. furosemide

31
Q

what do potassium sparing diuretics do? give an example and side-effects

A

increase excretion of sodium, water, chloride and calcium
decrease excretion of potassium and hydrogen ions
side- effects - ▪ dizziness, orthostatic hypotension
▪ dry mouth
▪ nausea, vomiting, diarrhea
e.g. amiloride

32
Q

what drugs are used to treat myocardial infarction?

A

anti-coagulants, A, B and C drugs

33
Q

name 2 anti-coagulants

A

warfarin and heparin

34
Q

warfarin

A

decreases the biological activity of clotting factors II, VII, IX, and X and anticoagulant proteins C and S
teratogen, vitamin K antagonist, warfarin metabolism affected by several drugs and food, monitored using INR - 2.5

35
Q

heparin

A

binds to antithrombin III which catalysts inactivation of factors IIa, Xa, IXa and XIIa
monitored using aPTT

36
Q

what are the side-effects of heparin? (4)

A
  • alopecia
  • hyperkalemia
  • hemorrhage/thrombocytopenia
  • osteoporosis
37
Q

name an anti-platelet drug

A

aspirin

38
Q

aspirin

A

inhibits cyclooxygenase, preventing formation of thromboxane A2

39
Q

what are the indications for aspirin?

A
  • acute coronary syndrome
  • acute stroke
  • prevention of cardiovascular disease
  • alternative to anti-coagulants in A.Fib
40
Q

what are the main drug groups used in treating asthma?

A

bronchodilators (relievers) and anti-inflammatory (controllers)

41
Q

give 3 examples of bronchodilators

A

B2 agonists, antimuscarinics and methylxanthines

42
Q

give 3 examples of anti-inflammatories

A

corticosteroids, lukasts and chromones

43
Q

what drugs are used to treat anaphylaxis and what do they do?

A

adrenaline - inhibits mast cell release of mediators
corticosteroids - reduce inflammation

44
Q

what do NSAIDs do?

A

they inhibit COX1 and COX2 which decreases prostaglandin synthesis
- anti-inflammatory
- analgesic
- anti-pyretic
- antiplatelet
- anti-tumour

45
Q

what are the side-effects of NSAIDs? (9)

A

headaches
dizziness
stomach pain
bone marrow toxicity
GI issues
hypersensitivity
liver damage
renal impairment
vascular disease

46
Q

what are the side-effects of opioids?

A

tolerance, dependance and withdrawal

47
Q

what are the consequences of alcohol use?

A
  • depressant -> causes disinhibition and dependence
    neuro: depression, stroke, neuropathy
    cardio: cardiomyopathy, hypertension
    resp: TB, pneumonia
    gastro: gastritis, ulcers, liver disease, pancreatitis
  • infertility, osteoporosis, cancers
48
Q

what are the consequences of cocaine use? (11)

A
  • psychosis
  • seizures
  • dysphoria
  • mydriasis
  • stroke
  • hyperthermia
  • tachycardia
  • heart attack
  • hypertension
  • kidney failure
  • blood coagulation
49
Q

what are the consequences of cannabis use?

A
  • impaired short-term memory
  • impaired motor coordination
  • altered judgement
  • paranoia/psychosis
  • addiction
  • altered brain development
  • cognitive impairment
  • diminished life satisfaction
  • risk of chronic psychosis disorders
50
Q

what are the principal drugs used in treating peptic ulcers?

A
  • antacids: neutralize acid and pepsin
  • alginates: prevents reflux
  • H2 receptor antagonists: reduce acid release
  • chelates: coats ulcer
  • proton pump inhibitors: reduce acid release and pepsin activation
51
Q

what are the principal drugs used in treating constipation?

A
  • bulk: increase fecal mass, promotes peristalsis (methylcellulose)
  • osmotic: increases water in large bowel (lactulose)
  • stimulants: increase intestinal motility (senna)
  • stool softeners: emollients (glycerol)
52
Q

what are the uses and action of nitrates?

A
  • used to treat angina and heart failure
  • relaxation of smooth muscle of veins and arterioles
    causes reduction in venous return (preload) which reduces left ventricular work. Arterioles also relax (afterload) rapid symptomatic relief of angina.
53
Q

what are the side effects of nitrates?

A

flushing, headache and postural hypotension