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SJ Phase 2a > Pharmacology > Flashcards

Pharmacology Flashcards

(73 cards)

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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
How do you thiazide diuretics work?
1. Inhibit Na+/Cl- contransporter in DCT 2. Less Na+ reabsorbed --> less water follows
26
How do K+ sparing diuretics work?
1. Inhibit reabsorption of Na+ and water in ENaC channels in DCT 2. Leads to Na+ and water excretion and K+ retention
27
Give examples of loop diuretics
1. Furosemide 2. Bumetanide
28
Give examples of thiazide diuretics
1. Bendroflumethiazide 2. Indapamide
29
Give examples of K+ sparing diuretics
1. Amiloride 2. Spironolactone - aldosterone antagonist but has same effect; blocking aldosterone --> ENaC blocked
30
Outline the mechanism of action of NSAIDs
1.Cyclooxygenase (COX) inhibitors --> Prevents production of prostoglandins (vasodilator) 2. COX-2 inhibition is useful, COX-1 inhibition causes adverse effects
31
Outline the mechanisms of action of antihistamines
1. H1 receptor antagonist 2. Prevents release of histamine from storage granules in mast cells
32
Outline the mechanisms of action of Proton Pump Inhibitor (PPI)
Irreversibly inhibits H+/K+-ATPase pump in gastric parietal cells to reduce proton secretion
33
Outline the mechanisms of action of opioids
Activation of muscarinic receptors in CNS
34
What is a common side effect of NSAIDS?
1. GI upset 2. GI bleed 3. Renal impairment
35
What is a common side effect of Anti-histamines?
1. Older ones can cross BBB and cause sedation 2. H1 receptors present in vomiting centre; can act as anti-emetics too.
36
What is a common side effect of ACE-inhibitor drugs?
1. Dry cough due to bradykinin as it induces sensitisation of airway sensory nerves 2. Dilates afferent glomerular arteriole; worsens kidney function
37
What is a common side effect of PPI?
Prolonged use in elderly leads to increased risk of fracture due to decreased calcium absorption --> osteoporosis
38
What is a common side effect of opioids?
1. Respiratory depression --> GIVE NALOXONE 2. Nausea and vomiting 3. Constipation 4. Tolerance and withdrawal
39
What is a common side effect of diuretics?
1. Spironolactone can cause hyperkalemia (K+ sparing) 2. Increased frequency of urination 3. Dehydration
40
What is the difference between side effects and adverse drug reactions?
1. Side effects = expected reaction 2. Adverse drug reactions = unexpected
41
What is the Yellow Card reporting scheme?
Allows reporting of all adverse drug reactions
42
Outline UMS of Alendronate/alendronic acid
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
Outline UMS of Atenolol
USE - treat hypertension and arrhythmia MECHANISM - beta 1 blocker SIDE EFFECTS 1. Bradycardia 2. Peripheral coldness 3. Lethargy
44
Outline UMS of Atracurium
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
Outline UMS of Bendroflumethiazide
USE - treat hypertension MECHANISM - thiazide diuretic SIDE EFFECTS 1. D&V 2. ED 3. Fatigue
46
Outline UMS of Cephuroxime
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
Outline UMS of Celecoxib
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
Outline UMS of Chloramphenicol
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
Outline UMS of Ciclosporin
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
Outline UMS of Ciprofloxacin
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
Outline UMS of Co-amoxiclav
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
Outline UMS of Diamorphine
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
Outline UMS of Dalteparin
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
Outline UMS of Dobutamine
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
Outline UMS of Doxazosin
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
Outline UMS of Ephedrine
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
Outline UMS of Erythromycin
USE - antibiotic MECHANISM OF ACTION 1. Protein synthesis inhibition 2. Bind to bacterial ribosome SIDE EFFECTS 1. D&V 2. Loss of appetite
58
Outline UMS oof Ethinylestradiol
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
Outline UMS of furosemide
USE - treat hypertension MECHANISM OF ACTION - loop diuretic SIDE EFFECTS 1. Dry mouth 2. N&V 3. Headaches
60
Outline UMS of Ipratropium
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
Outline UMS of Loperamide
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
Outline UMS of Metformin
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
Outline UMS of methotrexate
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
outline UMS of Oxybutynin
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
Outline UMS of Paracetamol
USE - analgesiac and antipyretic MECHANISM OF ACTION - COX inhibitor --> prosoglandins synthesis reduced --> pain relief SIDE EFFECTS 1. Allergic reaction
66
Outline UMS of Ramipril
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
Outline UMS of Rifampicin
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
Outline UMS of Rivaroxaban
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
Outline UMS of Salmeterol
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
Outline UMS of Sildenafil
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
Outline UMS of Suxamethonium
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
Outline UMS for Tamsulosin
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
Outline UMS of Tramadol
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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