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Phase 2a > ICS - Pharmacology > Flashcards

ICS - 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 ulcers

ACEi 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
What is the difference between the sympathetic and parasympathetic nervous system?
Sympathetic - fight or flight (increased HR, bronchodilation, decreased GI mobility). Parasympathetic - rest and digest (decreased HR, bronchoconstriction, increased GI mobility).
26
What is the difference between cholinergic and adrenergic pharmacology?
Cholinergic - parasympathetic Adrenergic - sympathetic
27
Describe the action of Ach at neuromuscular junctions.
Synthesis, vesicle storage, release, breakdown, reuptake.
28
What is an example of a drug at neuromuscular junctions (cholinergic)?
Botox - Ach release is inhibited resulting in paralysis.
29
What is the name of overstimulation of Ach and nmj's and what are the symptoms?
Cholinergic crisis (SLUDGE): Salivation, lacrimation, urination, defaecation, GI distress and emesis.
30
What are three examples of Ach receptors?
M1 - Brain M2 - Heart M3 - Lungs
31
How is adrenaline formed?
Tyrosine - DOPA - Dopamine - Noradrenaline - Adrenaline.
32
What are the types of noradrenaline receptors?
Alpha or beta (a1, a2, b1, b2).
33
Where are alpha-1 receptors found and what does the agonism cause? Give an example.
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.
34
Where are beta-1 receptors found and what are the examples of drugs?
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)
35
Where are beta-2 receptors found and what are the examples of drugs here?
Found in the lungs. Agonism causes bronchodilation. SABAs and LABAs are beta agonists (for asthma). Non-selective beta blockers are antagonists (propranolol).
36
What are examples of dopamine receptor agonists/antagonists?
Agonists (bromocriptine) - Used in prolactinoma, acromegaly and early Parkinson's. Antagonists (metoclopramide) - Anti-emetic, often used for nausea and vomiting.
37
What is an example of a GABA receptor agonist?
Benzodiazepines - Such as larazepam and diazepam. Used for anxiety, sleep disorders and alcohol withdrawal.
38
What are examples of histamine antagonists?
H1 antagonists - For allergy (loraditine) H2 antagonists - 2nd line Tx for GORD/increased gastric acid after PPIs (ranitidine).
39
What is an adverse drug reaction?
A response to a medicine which is noxious and unintended.
40
What are the five types of adverse drug reactions?
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
What is the method of reporting new adverse drug reactions?
Yellow card scheme.
42
What are some examples of opioids?
Morphine, codeine (weak). Diamorphine (heroin) Oral bioavailability is 50%
43
What is the potency of some opioids compared?
For the same effect: 5mg diamorphine 10mg morphine 100mg pethidine
44
What is the use of opioids and their side effects?
Used for chronic severe pain (analgesia). Side effects = Addiction, N+V, constipation and respiratory distress.
45
What is the difference between tolerance and dependence?
Tolerance: Reduced reaction to drug due to overstimulation of opioid receptor (desensitisation). Dependence: Psychological state of craving euphoria.
46
What is the treatment for opioid induced respiratory depression?
Naloxone - competitive opioid inhibitor
47
What is the action of NSAIDs?
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
What is the action of antihistamines?
H1 receptor antagonist - prevents histamine release from storage granules in mast cells which causes allergic reaction symptoms.
49
What is the action of ACE inhibitors?
Block action of ACE which prevents angiotensin I from being converted to angiotensin II, no aldosterone and no vasodilation. -Decreases blood pressure.
50
What is the action of PPIs?
Inhibits H+/K+ ATPase pump in gastric parietal cells to reduce H+ secretion.
51
What types of diuretics is there?
Loop, thiazide, K+ sparing.
52
What is the action of loop diuretics?
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
What is the action of thiazide diuretics?
Inhibits Na+/Cl- cotransporter in DCT - less Na+ reabsorbed so less water is reabsorbed.
54
What is the action of K+ sparing diuretics?
Inhibits reabsorption of Na+ and water in ENaC channels in DCT - leads to Na+ and water excretion and K+ retention.
55
What is the action of antiplatelet drugs?
Aspirin - COX1 inhibition (decreased thromboxane A2, this activates platelets). Clopidogrel - P2Y12 inhibition which affects thromboxane A2.
56
What is the action of four anticoagulant drugs?
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
What is a common side effect of NSAIDs?
Peptic ulcers - GI bleeding
58
What is a common side effect of ACE inhibitors?
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
What is a common side effect of PPIs?
Prolonged use can increase fracture risk.
60
What is a common side effect of anti-histamines?
Can cross BBB - causes sedation. Can also act as an anti-emetic as there are many H1 receptors in vomiting centre.
61
What is a common side effect of opioids?
Respiratory distress, tolerance, dependence, N+V. Tx - Naloxone. Reverses effects of opioids.
62
What are common side effects of loop and thiazide diuretics?
Hypokalaemia and dehydration.
63
What are common side effects of K+ sparing diuretics?
Treats oedema. Can cause hyperkalaemia.
64
What are the common side effects of beta blockers?
Bradycardia, dizziness, lightheadedness, cold extremeties.
65
What are common side effects of calcium channel blockers?
Ankle swelling, flushing, palpatations.
66
What are common side effects of steroids?
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
Which antibiotics are used for community-acquired pneumonia (CAP)?
Amoxicillin/co-amoxiclav - TYPICAL (s. pneumoniae) Clarythromycin - ATYPICAL (legionella, c. pneumoniae, m. pneumoniae)
68
Which antibiotics are used for hospital-acquired pneumonia?
Co-amoxiclav
69
Which antibiotics are used for COPD?
Amoxicillin, clarythromycin, doxycycline.
70
Which antibiotics are used for TB?
RIPE: Rifampicin, isoniazid, pyramizine, ethambutol.
71
Which antibiotics are used for cellulitis?
Flucloxacillin - mostly B strep or s. aureus. Vancomycin - MRSA
72
Which antibiotics are used for UTIs?
Trimethoprim and nitrofurantoin. -Cefalexin for pregnancy.
73
Which antibiotics are used for pyelonephritis?
Cefalexin and co-amoxiclav.
74
Which antibiotics are used for chlamydia?
Azithromycin and doxycycline.
75
Which antibiotics are used for gonorrhoea?
IM ceftriaxone and azithromycin.
76
Which antibiotics are used for syphilis?
Benzathine penicillin and benzylpenicillin.
77
Which antibiotics are used for helicobacter pylori?
Claythromycin, amoxicillin, metronidazole. PPIs may also be used to treat potential stomach ulcers.
78
Which antibiotics are used for gastroenteritis?
If bacterial: Clarythromycin - campylobacter Ciprofloxacin - salmonella and shigella
79
Which antibiotics are used for C. diffcile?
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
Which antibiotics are used to treat infective endocarditis?
Vancomycin and rifampicin if s. aureus. Benzylpenicillin and gentamycin if s. viridans.
81
What is a receptor?
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
What are the different forms of ligands?
Exogenous (drugs) and endogenous (hormones, neurotransmitters).
83
What are the different types of receptors?
Ligand-gated ion channels, G coupled protein receptors, kinase-linked receptors, cytosolic receptors.
84
What is an example of a ligand-gated ion channel?
Nicotinic Ach receptor.
85
What is an example of a G-coupled receptor?
Beta-adrenoreceptors.
86
What is an example of a kinase-linked receptor?
Receptors for growth factors.
87
What is an example of a cytosolic receptor?
Steroid receptors.
88
Give an example of enteral drug administrations?
Oral and rectal.
89
Describe the affinity and efficacy of an agonist.
Full affinity and full efficacy.
90
Describe the affinity and efficacy of an antagonist.
Full affinity and zero efficacy.
91
Describe the graph changes of a competitive inhibitor.
Curve shifts right: -Drug has less affinity but same efficacy. -Drug is less potent.
92
Describe the graph changes of a non-competitive inhibitor.
Curve shifts right and down: -Drug has less affinity and less efficacy. -Drug is less potent.
93
What is therapeutic range?
Upper and lower bounds of safe doses of a drug.
94
What are the main receptors of cholinergic pharmacology?
Nicotinic and muscarinic.
95
What are opioids used for?
Chronic severe pain relief.
96
Describe the pain ladder.
Mild - Weak analgesia (paracetamol, NSAIDs). Moderate - Moderate analgesia (codeine, tramadol). Severe - Severe analgesia (morphine, diamorphine).
97
Describe the metabolism for paracetamol.
Undergoes phase II hepatic metabolism 95% and phase 1 for 5%.
98
How does paracetamol overdose present?
Fulminant liver failure and shutting down of physiological systems.

Phase 2a (14 decks)

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