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SJ Phase 2a > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is pharmacodynamics?

A

What the drug does to the body
-Affinity
-Efficacy
-Potency

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2
Q

What is pharmacokinetics

A

What the body does to the drug (ADME)
- Absorption
- Distribution
- Metabolism
- Excretion

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3
Q

What is drug affinity?

A

The capacity for a drug to bind to a receptor

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4
Q

What is drug efficacy?

A

The maximum effect a drug can have win the body

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5
Q

What is drug potency?

A

How much drug is needed to elicit a response in the body

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6
Q

What is the mechanism of an agonist drug?

A

Attaches to and stimulate receptor

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7
Q

What is the mechanism of a competitive inhibitor?

A

Block receptor site

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8
Q

What is the mechanism of a non-competitive inhibitor?

A

alters receptor action site to prevent binding by binding at a site different to the action site

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9
Q

What is bioavailability?

A

The proportion of the drug given that enters circulation and can exert effect on body

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10
Q

What is first pass metabolism?

A

reduction of drug concentration due to metabolism by the body, especially the liver

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11
Q

State the main routes of administration of drugs and properties

A
  1. Oral - first pass metabolism
  2. IV - directly into systemic circulation
  3. Subcutaneous - has to diffuse through subcutaneous fat; absorbs slowly
  4. Intramuscular - Muscle = high vascularity so rapid absorption
  5. Topical - Directly onto skin/mucosa. Avoids first pass metabolism, slow absorption into circulation
  6. Rectal - Used when patient unable to tolerate oral route. Highly vascular so rapid absorption
  7. Intrathecal (into spinal column) - Direct access to CSF
  8. Sublingual/buccal (under the tongue) - Avoids first pass metabolism, rapid circ. absorption
  9. Inhalation - Effective if lung is target site
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12
Q

What is the function of eGFR and CrCl

A

Test of kidney function

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13
Q

What is CrCl?

A

Volume of blood plasma cleared of creatinine per unit time. Used to estimate GFR. Done by comparing serum creatinine vs urine creatinine.

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14
Q

Why is kidney function relevant when prescribing drugs?

A
  1. Most drugs excreted by kidneys
  2. Impaired kidney function –> reduced renal excretion of drug
  3. Drug concentration builds up –> toxicity and possible further renal impairment
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15
Q

Give examples of conditions where drugs would need to be adjusted to account for impaired kidney function

A
  1. CKD
  2. AKI
  3. Diabetes
  4. HTN (hypertension)
  5. Polycystic kidney disease
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16
Q

What does the Beta1 receptor act on and how?

A
  1. Heart - increased CO
  2. Kidneys - increased renin
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17
Q

What does the Beta2 receptor act on and how?

A

-Smooth muscle relaxation
1. Lungs - expansion
2. Blood vessels - dilated
3. GI tract - Peristaltic digestion decrease
4. Bladder - Urination decrease
5. Uterus - relaxation of uterine muscles
6. Liver - glycogenolysis; glucose released from liver to muscle

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18
Q

What does the Beta3 receptor act on and how?

A
  1. Adipose tissue - lipolysis and thermogenesis
  2. Bladder - decrease urination
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19
Q

What does the Alpha1 receptor act on and how?

A

-smooth muscle contraction
1. Blood vessels - contract
2. Pupils - dilate
3. Pylorus - contract
4. Urinary sphincter - contract
5. Prostate - contract

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20
Q

What does Alpha2 receptor act on and how?

A

-inhibitory
1. Presynaptic nerve terminals - inhibition

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21
Q

What receptors does the sympathetic NS act on?

A
  1. Alpha 1
  2. Alpha 2
  3. Beta 1
  4. Beta 2
  5. Beta 3
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22
Q

What receptors does the parasympathetic NS act on?

A

Muscarinic receptors

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23
Q

What are the 3 main types of diuretics?

A
  1. Loop diuretics
  2. Thiazide diuretics
  3. K+ sparing diuretics
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24
Q

How do loop diuretics work?

A
  1. Inhibit Na+/K+/Cl- cotransporters
  2. Normally all 3 ions absorbed, drawing water back into vasculature
  3. Blocked –> less water reabsorbed
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25
Q

How do you thiazide diuretics work?

A
  1. Inhibit Na+/Cl- contransporter in DCT
  2. Less Na+ reabsorbed –> less water follows
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26
Q

How do K+ sparing diuretics work?

A
  1. Inhibit reabsorption of Na+ and water in ENaC channels in DCT
  2. Leads to Na+ and water excretion and K+ retention
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27
Q

Give examples of loop diuretics

A
  1. Furosemide
  2. Bumetanide
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28
Q

Give examples of thiazide diuretics

A
  1. Bendroflumethiazide
  2. Indapamide
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29
Q

Give examples of K+ sparing diuretics

A
  1. Amiloride
  2. Spironolactone - aldosterone antagonist but has same effect; blocking aldosterone –> ENaC blocked
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30
Q

Outline the mechanism of action of NSAIDs

A

1.Cyclooxygenase (COX) inhibitors –> Prevents production of prostoglandins (vasodilator)
2. COX-2 inhibition is useful, COX-1 inhibition causes adverse effects

31
Q

Outline the mechanisms of action of antihistamines

A
  1. H1 receptor antagonist
  2. Prevents release of histamine from storage granules in mast cells
32
Q

Outline the mechanisms of action of Proton Pump Inhibitor (PPI)

A

Irreversibly inhibits H+/K+-ATPase pump in gastric parietal cells to reduce proton secretion

33
Q

Outline the mechanisms of action of opioids

A

Activation of muscarinic receptors in CNS

34
Q

What is a common side effect of NSAIDS?

A
  1. GI upset
  2. GI bleed
  3. Renal impairment
35
Q

What is a common side effect of Anti-histamines?

A
  1. Older ones can cross BBB and cause sedation
  2. H1 receptors present in vomiting centre; can act as anti-emetics too.
36
Q

What is a common side effect of ACE-inhibitor drugs?

A
  1. Dry cough due to bradykinin as it induces sensitisation of airway sensory nerves
  2. Dilates afferent glomerular arteriole; worsens kidney function
37
Q

What is a common side effect of PPI?

A

Prolonged use in elderly leads to increased risk of fracture due to decreased calcium absorption –> osteoporosis

38
Q

What is a common side effect of opioids?

A
  1. Respiratory depression –> GIVE NALOXONE
  2. Nausea and vomiting
  3. Constipation
  4. Tolerance and withdrawal
39
Q

What is a common side effect of diuretics?

A
  1. Spironolactone can cause hyperkalemia (K+ sparing)
  2. Increased frequency of urination
  3. Dehydration
40
Q

What is the difference between side effects and adverse drug reactions?

A
  1. Side effects = expected reaction
  2. Adverse drug reactions = unexpected
41
Q

What is the Yellow Card reporting scheme?

A

Allows reporting of all adverse drug reactions

42
Q

Outline UMS of Alendronate/alendronic acid

A

USE - treat osteoporosis
MECHANISM
1. Bisphosphonate adsorbed onto hydroxyapatite crystals in bone
2. Slows rate if growth and dissolution
3. reduces rate of bone turnover
SIDE EFFECT
1. D&V
2. Electrolyte imbalance
3. Change in ability to taste food

43
Q

Outline UMS of Atenolol

A

USE - treat hypertension and arrhythmia
MECHANISM - beta 1 blocker
SIDE EFFECTS
1. Bradycardia
2. Peripheral coldness
3. Lethargy

44
Q

Outline UMS of Atracurium

A

USE - neuromuscular blockade for surgery and mechanical ventilation
MECHANISM - Blocking the action of Ach on skeletal muscles
SIDE EFFECTS
1. Flushing
2. Hypotension
3. Bronchospasm

45
Q

Outline UMS of Bendroflumethiazide

A

USE - treat hypertension
MECHANISM - thiazide diuretic
SIDE EFFECTS
1. D&V
2. ED
3. Fatigue

46
Q

Outline UMS of Cephuroxime

A

USE - antibacterial
MECHANISM
1. attach to penicillin binding protein
2. Interrupts cell wall biosynthesis
3. Bacteria death
SIDE EFFECTS
1. D&V
2. Thrombocytopenia

47
Q

Outline UMS of Celecoxib

A

USE - COX-2 inhibitor; treat pain and inflammation in osteoarthritis and rheumatoid arthritis
MECHANISM - SELECTIVE INHIBITION OF COX-2
SIDE EFFECTS
1. Gas/bloating
2. Constipation
3. Flu like symptoms

48
Q

Outline UMS of Chloramphenicol

A

USE - antibiotic, used for eye infections
MECHANISM - Inhibit microbial protein synthesis by binding to microbial ribosome
SIDE EFFECTS
1. Stinging
2. Burning sensation
3. Irritation

49
Q

Outline UMS of Ciclosporin

A

USE
1. treat pain in rheumatoid arthirtis
2. Prevent rejection of transplanted organ
MECHANISM
Inhibit synthesis of interleukins which are used for self-activation of T lymphocytes
SIDE EFFECTS
1. High BP
2. Increased hair growth
3. Swollen gums

50
Q

Outline UMS of Ciprofloxacin

A

USE - Treat many serious infectious bacterial diseases such as
1. Pneumonia
2. Typhoid
3. Gonorrhea
MECHANISM - bacterial topoisomerase inhibitor
SIDE EFFECTS
1. D&V
2. Stomach pain
3. Lethargy

51
Q

Outline UMS of Co-amoxiclav

A

USE - antibiotic
MECHANISM
1. Amoxicillin + clavulanic acid
2. Acid prevents bateria breaking down amox
3. Amoxicillin works like penicillin; bind to penicillin-bnding proteins to prevent cell wall synthesis
SIDE EFFECTS
1. D&V
2. Thrush

52
Q

Outline UMS of Diamorphine

A

USE
1. Analgesia
2. MI
3. Respiratory sedative
MECHANISM OF ACTION
1. mu-opiod agonist
2. Acts on mu-opioid receptors in CNS & PNS
SIDE EFFECTS
1. Sweating
2. N&V
3. Constipation

53
Q

Outline UMS of Dalteparin

A

USE - anticoagulant
MECHANISM OF ACTION
1. Increase activity of antithrombin III
2. Thus formation of factor Xa and thrombin prevented
SIDE EFFECTS
1. Excessive bleeding
2. Diarrhoea
3. Jaundice

54
Q

Outline UMS of Dobutamine

A

USE - short term cardiac stimulant to increase contractility; manage low BP
MECHANISM OF ACTION
1. Stimulate beta-1 receptors in the heart
2. Increase myocardial contractility
3. Increased CO
SIDE EFFECTS
1. Dyspnea (shortness of breath)
2. Chest pain
3. Rapid weight gain

55
Q

Outline UMS of Doxazosin

A

USE
1. Treat hypertension
2. Reduce symptoms of enlarged prostate
MECHANISM OF ACTION
1. Alpha-1 receptor blocker
2. decreases peripheral vascular resistance; BP decreased
SIDE EFFECTS
1. Oedema in peripheries
2. UTI
3. Headaches

56
Q

Outline UMS of Ephedrine

A

USE
1. Treat hypotension during anesthesia
2. Bronchial asthma
MECHANISM OF ACTION
1. Alpha1, beta1 and beta2 adrenergic receptors agonist
2. Increased stimulation of sympathetic nervous system
SIDE EFFECTS
1. Blurred vision
2. Arrhytmia
3. Nausea

57
Q

Outline UMS of Erythromycin

A

USE - antibiotic
MECHANISM OF ACTION
1. Protein synthesis inhibition
2. Bind to bacterial ribosome
SIDE EFFECTS
1. D&V
2. Loss of appetite

58
Q

Outline UMS oof Ethinylestradiol

A

USE
1. Oestrogen deficiency
2. Menstrual disorders
3. Prostate cancer
4. Contraception
MECHANISM OF ACTION
1. Synthetic estrogen
2. Decreases LH –> prevent ovulation
SIDE EFFECTS
1. Peripheral oedema
2. N&V
3. Weight change

59
Q

Outline UMS of furosemide

A

USE - treat hypertension
MECHANISM OF ACTION - loop diuretic
SIDE EFFECTS
1. Dry mouth
2. N&V
3. Headaches

60
Q

Outline UMS of Ipratropium

A

USE - Bronchodilator; COPD symptom control
MECHANISM OF ACTION
1. Ach antagonist via block of muscarinic cholinergic receptor
2. Inhibit parasympathetic nervous system; decreased smooth muscle contraction in lungs
SIDE EFFECTS
1. Bladder pain
2. Painful urination
3. Dry mouth

61
Q

Outline UMS of Loperamide

A

USE - treat diarrhoea
MECHANISM OF ACTION
1. Acts on mu-opiod receptor in intestinal muscle
2. Inhibits release of Ach and prostoglandins; propulsive peristalsis reduced, intenstinal transit time increased
3. Stimulate intestinal water absorption
SIDE EFFECTS
1. Constipation
2. Dizzy

62
Q

Outline UMS of Metformin

A

USE - Type II diabetes
MECHANISM OF ACTION
1. Decrease hepatic glucosneogenesis
2. Decrease Intestinal absorption of glucose
SIDE EFFECTS
1. D&V
2. Loss of appetite

63
Q

Outline UMS of methotrexate

A

USE
1. Treat cancer
2. Rheumatoid arthiritis
MECHANISM OF ACTION
1. Inhibit enzymes responsible for nucleotide synthesis; prevents cell division
SIDE EFFECTS
1. D&V
2. Mouth ulcers
3. Hair loss

64
Q

outline UMS of Oxybutynin

A

USE - treat overactive bladder
MECHANISM OF ACTION
1. relax bladder
2. Inhibit muscarinic action of Ach on smooth muscle
SIDE EFFECTS
1. D&V
2. Dry mouth
3. Vertigo

65
Q

Outline UMS of Paracetamol

A

USE - analgesiac and antipyretic
MECHANISM OF ACTION - COX inhibitor –> prosoglandins synthesis reduced –> pain relief
SIDE EFFECTS
1. Allergic reaction

66
Q

Outline UMS of Ramipril

A

USE - treat hypertension
MECHANISM OF ACTION
1. ACE inhibitor
2. Inhibit RAAS system
3. Prevent angiotensin I to II conversion
SIDE EFFECTS
1. D&V
2. Headaches
3. Dry cough

67
Q

Outline UMS of Rifampicin

A

USE - antibiotic to treat TB
MECHANISM OF ACTION
1. Inhibition of DNA dependent RNA polymerase
2. RNA synthesis supression
SIDE EFFECTS
1. Temporary discoloration of skin
2. Drowsiness
3. Vertigo

68
Q

Outline UMS of Rivaroxaban

A

USE - Treat and prevent DVT
MECHANISM OF ACTION
1. Anticoagulant that finds directly to factor Xa
2. Blocks coagulation cascade amplification
SIDE EFFECTS
1. Bleeding
2. Lethargy
3. N&V

69
Q

Outline UMS of Salmeterol

A

USE - Control symptoms of asthma and prevent bronchospasms
MECHANISM OF ACTION
1. Beta2 adrenoreceptor agonist
2. Causes bronchorelaxation
SIDE EFFECTS
1. Dry mouth
2. D&V
3. Trembling

70
Q

Outline UMS of Sildenafil

A

USE - treat ED
MECHANISM OF ACTION
Increased blood flow to penis by enhancing effect of NO on corpus cavernosum
SIDE EFFECTS
1. Stuffy nose
2. Nausea
3. Headache

71
Q

Outline UMS of Suxamethonium

A

USE - anaesthesia for intubation and mechanical ventilation
MECHANISM OF ACTION
1. Skeletal muscle relaxant
2. Mimics Ach at neuromuscular junction, but slowed hydrolysis
3. Results in prolonged depolarisation by blockade
4. Results in skeletal muscle paralysis
SIDE EFFECTS
1. Myalgia
2. Arrhytmia
3. Hyperthermia

72
Q

Outline UMS for Tamsulosin

A

USE - treat enlarged prostate
MECHANISM OF ACTION
1. Alpha1 adrenoreceptoor blocker
2. Relaxes smooth muscle in prostate
SIDE EFFECTS
1. Back pain
2. Flu like symptoms
3. Sleeping difficulties

73
Q

Outline UMS of Tramadol

A

USE - Opioid analgesiac
MECHANISM OF ACTION
1. mu-receptor agonist
2. SNRI (serotonin/norepinepherine reuptake-inhibitor)
SIDE EFFECTS
1. Dry mouth
2. Sweating
3. Constipation

SJ Phase 2a (13 decks)

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