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ICS > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What are the routes of administration of drugs?

A

Enteral (GI tract):-Oral, rectal.Perienteral (Non-gut):-IV, IM, SC.

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2
Q

What is first pass metabolism?

A

When the drug is administered orally its concentration is reduced due to the liver or gut metabolising it before reaching systemic circulation.

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3
Q

What is bioavailability?

A

The amount of drug taken up as a proportion of the amount administered.

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4
Q

What is potency?

A

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

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5
Q

What is the difference between affinity and efficacy?

A

Affinity describes how well a ligand binds to the receptor.Efficacy describes how well a ligand activates the receptor.

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6
Q

What is the difference between selectivity and specificity?

A

Selectivity - A drug’s ability to discriminate between related targets.Specificity - The measure of a receptors ability to respond to a single ligand.

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7
Q

What is an agonist?

A

A compound that binds to a receptor and activates it.

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8
Q

What is an antagonist?

A

A compound that reduces the effect of an agonist.

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9
Q

What are the types of antagonists and how do they differ?

A

Competitive inhibitors - Compete with substrate for active site.Non-competitive inhibitors - Bind away from active site to denature it so no substrate can bind in it.

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10
Q

What four things do drugs target?

A

Receptors, enzymes, transporters, ion channels.

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11
Q

What are the most common receptors?

A

G-coupled receptors.

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12
Q

What are examples of selective and non-selective drugs?

A

Beta blockers:Propranolol - Non-selective b-blocker; binds to both b-1 and b-2.Bisoprolol - Selective b-blocker; binds to b-1.

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13
Q

What drugs are examples of beta-adrenergic agonists? (selective and non-selective).

A

Non-selective beta agonist: Isoprenaline (b-1 and b-2).Selective beta agonist: SABAs (b-2).

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14
Q

What are the main examples of drugs that target enzymes?

A

COX-1 and ACEi:NSAIDs inhibits cox-1 which prevents arachidonic acid which inhibits prostaglandins. SE = GI ulcersACEi inhibits angiotensin-1 to angiotensin-2. SE = Hyperkalaemia, dry cough.

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15
Q

What are the main examples of drugs that target transporters?

A

Mainly PPIs and diuretics.PPIs: Omeprazole - inhibition of H+/K+ ATPase pumps (decreased gastric pH).Diuretics: -Loop (furosemide) - Inhibits NKCC2 symporter in ascending limb of loop of Henle.-Thiazides (bendroflumethiazide) - Inhibits NaCl cotransporter in DCT.-K+ sparing (spironolactone) - Inhibits aldosterone.

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16
Q

What are the main examples of drugs that inhibit ion channels?

A

CCBs and local anaesthesia.CCBs such as amiodarone and verapamil. Ca2+ influx causes vasoconstriction and increased contractility which is blocked.Local anaesthesia such as lidocaine block Na+ voltage gated channels - no fast Na_ influx and no action potential.

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17
Q

What is the definition of pharmacokinetics?

A

What the body does to the drug (ADME).

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18
Q

What are the four factors of pharmacokinetics?

A

ADME - Absorption, distribution, metabolism and excretion.

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19
Q

Describe absorption in pharmacokinetics.

A

Route and entry of drug into body. Enteral vs perienteral.The bioavailability of IV is always 100%. Other routes are compared to IV. Oral medications have to undergo first pass metabolism - reduces bioavailability.

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20
Q

Describe distribution in pharmacokinetics.

A

The drug is distributed in plasma according to chemical properties and size. May be uptaken by organs (liver and brain).This is affected by blood flow, size, lipophilic/lipophobic.

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21
Q

Describe metabolism in pharmacokinetics.

A

Drugs are mainly metabolised in the kidneys and liver. In liver there are phase I (slight hydrophilicity increase by microsomal enzymes) and phase II (hydrophilicity increased by conjugation).Kidneys - mostly small and water soluble.Liver - hydrophobic molecules.

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22
Q

Describe excretion in pharmacokinetics.

A

Mostly excreted in urine by kidneys and faeces.

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23
Q

What is pharmacodynamics?

A

What the drug does to the body.

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24
Q

What is the difference between the sympathetic and parasympathetic nervous system (neurotransmitters)?

A

Sympathetic - Noradrenaline.Parasympathetic- Acetylcholine.

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25
Q

What is the difference between the sympathetic and parasympathetic nervous system?

A

Sympathetic - fight or flight (increased HR, bronchodilation, decreased GI mobility).Parasympathetic - rest and digest (decreased HR, bronchoconstriction, increased GI mobility).

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26
Q

What is the difference between cholinergic and adrenergic pharmacology?

A

Cholinergic - parasympatheticAdrenergic - sympathetic

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27
Q

Describe the action of Ach at neuromuscular junctions.

A

Synthesis, vesicle storage, release, breakdown, reuptake.

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28
Q

What is an example of a drug at neuromuscular junctions (cholinergic)?

A

Botox - Ach release is inhibited resulting in paralysis.

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29
Q

What is the name of overstimulation of Ach and nmj’s and what are the symptoms?

A

Cholinergic crisis (SLUDGE):Salivation, lacrimation, urination, defaecation, GI distress and emesis.

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30
Q

What are three examples of Ach receptors?

A

M1 - BrainM2 - HeartM3 - Lungs

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31
Q

How is adrenaline formed?

A

Tyrosine - DOPA - Dopamine - Noradrenaline - Adrenaline.

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32
Q

What are the types of noradrenaline receptors?

A

Alpha or beta (a1, a2, b1, b2).

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33
Q

Where are alpha-1 receptors found and what does the agonism cause? Give an example.

A

Found in vessels and sphincters.Agonism causes vasoconstriction, bladder contraction and pupil dilation.Alpha blockers (tamsulosin) are a treatment for benign prostate hyperplasia as this relaxes the bladder and eases pressure.

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34
Q

Where are beta-1 receptors found and what are the examples of drugs?

A

Found in the heart.Agonism causes increased force of contraction and increased blood pressure. Beta-1 agonists - given in cardiogenic shock (dobutamine).Beta-1 antagonists - bisoprolol (beta-blocker)

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35
Q

Where are beta-2 receptors found and what are the examples of drugs here?

A

Found in the lungs.Agonism causes bronchodilation.SABAs and LABAs are beta agonists (for asthma).Non-selective beta blockers are antagonists (propranolol).

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36
Q

What are examples of dopamine receptor agonists/antagonists?

A

Agonists (bromocriptine) - Used in prolactinoma, acromegaly and early Parkinson’s.Antagonists (metoclopramide) - Anti-emetic, often used for nausea and vomiting.

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37
Q

What is an example of a GABA receptor agonist?

A

Benzodiazepines - Such as larazepam and diazepam. Used for anxiety, sleep disorders and alcohol withdrawal.

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38
Q

What are examples of histamine antagonists?

A

H1 antagonists - For allergy (loraditine) H2 antagonists - 2nd line Tx for GORD/increased gastric acid after PPIs (ranitidine).

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39
Q

What is an adverse drug reaction?

A

A response to a medicine which is noxious and unintended.

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40
Q

What are the five types of adverse drug reactions?

A

Augmented (exaggerated action at normal dose).Bizarre (new responses not expected).Chronic (persist for a long time).Delayed (effect comes after a while).End of use (associated with withdrawal).

41
Q

What is the method of reporting new adverse drug reactions?

A

Yellow card scheme.

42
Q

What are some examples of opioids?

A

Morphine, codeine (weak).Diamorphine (heroin)Oral bioavailability is 50%

43
Q

What is the potency of some opioids compared?

A

For the same effect:5mg diamorphine10mg morphine100mg pethidine

44
Q

What is the use of opioids and their side effects?

A

Used for chronic severe pain (analgesia).Side effects = Addiction, N+V, constipation and respiratory distress.

45
Q

What is the difference between tolerance and dependence?

A

Tolerance: Reduced reaction to drug due to overstimulation of opioid receptor (desensitisation).Dependence: Psychological state of craving euphoria.

46
Q

What is the treatment for opioid induced respiratory depression?

A

Naloxone - competitive opioid inhibitor

47
Q

What is the action of NSAIDs?

A

Inhibits cox-1 and cox-2 which prevents prostaglandin production.Cox-1 inhibition causes adverse side effects (decreased gastric mucosal protection).Cox-2 inhibition is useful as it is anti-inflammatory.

48
Q

What is the action of antihistamines?

A

H1 receptor antagonist - prevents histamine release from storage granules in mast cells which causes allergic reaction symptoms.

49
Q

What is the action of ACE inhibitors?

A

Block action of ACE which prevents angiotensin I from being converted to angiotensin II, no aldosterone and no vasodilation.-Decreases blood pressure.

50
Q

What is the action of PPIs?

A

Inhibits H+/K+ ATPase pump in gastric parietal cells to reduce H+ secretion.

51
Q

What types of diuretics is there?

A

Loop, thiazide, K+ sparing.

52
Q

What is the action of loop diuretics?

A

Inhibits Na+/K+/Cl- (NKCC2) transporters - when these are absorbed water follows but as it is blocked there’s less water absorbed and more excreted.-Furosemide.

53
Q

What is the action of thiazide diuretics?

A

Inhibits Na+/Cl- cotransporter in DCT - less Na+ reabsorbed so less water is reabsorbed.

54
Q

What is the action of K+ sparing diuretics?

A

Inhibits reabsorption of Na+ and water in ENaC channels in DCT - leads to Na+ and water excretion and K+ retention.

55
Q

What is the action of antiplatelet drugs?

A

Aspirin - COX1 inhibition (decreased thromboxane A2, this activates platelets).Clopidogrel - P2Y12 inhibition which affects thromboxane A2.

56
Q

What is the action of four anticoagulant drugs?

A

Heparin - Activates antithrombin III and inactivates thrombin and factor Xa.Warfarin - Inhibits vitamin K dependent clotting factors (II, VII, IX, X).DOACs - (apixaban). Anti-factor Xa.Fibrinolytics - (alteplase). Activates plasmin to degrade fibrin.

57
Q

What is a common side effect of NSAIDs?

A

Peptic ulcers - GI bleeding

58
Q

What is a common side effect of ACE inhibitors?

A

Dry cough due to bradykinin accumulation in lungs. If this happens switch to angiotensin receptor blockers (ARBs).Can lead to acute kidney injury (AKI) due to the decreased GFR because of a dilated afferent arteriole.

59
Q

What is a common side effect of PPIs?

A

Prolonged use can increase fracture risk.

60
Q

What is a common side effect of anti-histamines?

A

Can cross BBB - causes sedation.Can also act as an anti-emetic as there are many H1 receptors in vomiting centre.

61
Q

What is a common side effect of opioids?

A

Respiratory distress, tolerance, dependence, N+V.Tx - Naloxone. Reverses effects of opioids.

62
Q

What are common side effects of loop and thiazide diuretics?

A

Hypokalaemia and dehydration.

63
Q

What are common side effects of K+ sparing diuretics?

A

Treats oedema. Can cause hyperkalaemia.

64
Q

What are the common side effects of beta blockers?

A

Bradycardia, dizziness, lightheadedness, cold extremeties.

65
Q

What are common side effects of calcium channel blockers?

A

Ankle swelling, flushing, palpatations.

66
Q

What are common side effects of steroids?

A

Glucocorticoids - CUSHINGOID MAP.Cataracts, ulcers, stretch marks, hypertension, increased infection risk, necrosis of bone, growth restriction, osteoporosis, increased ICP, DMT2, myopathy, adipose hypertrophy, pancreatitis.

67
Q

Which antibiotics are used for community-acquired pneumonia (CAP)?

A

Amoxicillin/co-amoxiclav - TYPICAL (s. pneumoniae)Clarythromycin - ATYPICAL (legionella, c. pneumoniae, m. pneumoniae)

68
Q

Which antibiotics are used for hospital-acquired pneumonia?

A

Co-amoxiclav

69
Q

Which antibiotics are used for COPD?

A

Amoxicillin, clarythromycin, doxycycline.

70
Q

Which antibiotics are used for TB?

A

RIPE: Rifampicin, isoniazid, pyramizine, ethambutol.

71
Q

Which antibiotics are used for cellulitis?

A

Flucloxacillin - mostly B strep or s. aureus.Vancomycin - MRSA

72
Q

Which antibiotics are used for UTIs?

A

Trimethoprim and nitrofurantoin.-Cefalexin for pregnancy.

73
Q

Which antibiotics are used for pyelonephritis?

A

Cefalexin and co-amoxiclav.

74
Q

Which antibiotics are used for chlamydia?

A

Azithromycin and doxycycline.

75
Q

Which antibiotics are used for gonorrhoea?

A

IM ceftriaxone and azithromycin.

76
Q

Which antibiotics are used for syphilis?

A

Benzathine penicillin and benzylpenicillin.

77
Q

Which antibiotics are used for helicobacter pylori?

A

Claythromycin, amoxicillin, metronidazole.PPIs may also be used to treat potential stomach ulcers.

78
Q

Which antibiotics are used for gastroenteritis?

A

If bacterial:Clarythromycin - campylobacterCiprofloxacin - salmonella and shigella

79
Q

Which antibiotics are used for C. diffcile?

A

This infection is usually caused by other antibiotics such as cephasporin, co-amoxiclav, ceftriaxone, cefalexin, cefotaxime, clindamycin. These antibiotics kill good bacteria allowing c. diff to multiply.Treat with vancomycin or metronidazole if severe.

80
Q

Which antibiotics are used to treat infective endocarditis?

A

Vancomycin and rifampicin if s. aureus.Benzylpenicillin and gentamycin if s. viridans.

81
Q

What is a receptor?

A

A component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to the ligands observed effects.

82
Q

What are the different forms of ligands?

A

Exogenous (drugs) and endogenous (hormones, neurotransmitters).

83
Q

What are the different types of receptors?

A

Ligand-gated ion channels, G coupled protein receptors, kinase-linked receptors, cytosolic receptors.

84
Q

What is an example of a ligand-gated ion channel?

A

Nicotinic Ach receptor.

85
Q

What is an example of a G-coupled receptor?

A

Beta-adrenoreceptors.

86
Q

What is an example of a kinase-linked receptor?

A

Receptors for growth factors.

87
Q

What is an example of a cytosolic receptor?

A

Steroid receptors.

88
Q

Give an example of enteral drug administrations?

A

Oral and rectal.

89
Q

Describe the affinity and efficacy of an agonist.

A

Full affinity and full efficacy.

90
Q

Describe the affinity and efficacy of an antagonist.

A

Full affinity and zero efficacy.

91
Q

Describe the graph changes of a competitive inhibitor.

A

Curve shifts right:-Drug has less affinity but same efficacy.-Drug is less potent.

92
Q

Describe the graph changes of a non-competitive inhibitor.

A

Curve shifts right and down:-Drug has less affinity and less efficacy.-Drug is less potent.

93
Q

What is therapeutic range?

A

Upper and lower bounds of safe doses of a drug.

94
Q

What are the main receptors of cholinergic pharmacology?

A

Nicotinic and muscarinic.

95
Q

What are opioids used for?

A

Chronic severe pain relief.

96
Q

Describe the pain ladder.

A

Mild - Weak analgesia (paracetamol, NSAIDs).Moderate - Moderate analgesia (codeine, tramadol).Severe - Severe analgesia (morphine, diamorphine).

97
Q

Describe the metabolism for paracetamol.

A

Undergoes phase II hepatic metabolism 95% and phase 1 for 5%.

98
Q

How does paracetamol overdose present?

A

Fulminant liver failure and shutting down of physiological systems.

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