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GEM > Drugs > Flashcards

Drugs Flashcards

1
Q

salbutamol

A

B2 agonist
Fast-acting for quick relief
e.g. asthma

Bronchodilation
Stabilise mast cells and inhibit inflammatory mediator release
Enhanced mucociliary clearance (action on cilia)

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2
Q

formoterol

A

B2 agonist
Formoterol acts quickly but has a long duration of action

Bronchodilation
Stabilise mast cells and inhibit inflammatory mediator release
Enhanced mucociliary clearance (action on cilia)

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3
Q

salmeterol

A

B2 agonist
Slower, longer lasting

Bronchodilation
Stabilise mast cells and inhibit inflammatory mediator release
Enhanced mucociliary clearance (action on cilia)

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4
Q

tiotropium

A

Muscarinic acetylcholine receptor antagonist
Long-acting “preventer”

Bronchodilation by antagonising action of ACh released by vagus nerve
↓ mucus secretion in asthma
↑ mucociliary clearance

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5
Q

Ipratropium

A

Muscarinic acetylcholine receptor antagonist
Fast-acting “reliever”

Bronchodilation by antagonising action of ACh released by vagus nerve
↓ mucus secretion in asthma
↑ mucociliary clearance

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6
Q

Atropine

A

Muscarinic acetylcholine receptor antagonist
Cannot cross membranes

Bronchodilation by antagonising action of ACh released by vagus nerve
↓ mucus secretion in asthma
↑ mucociliary clearance

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7
Q

theophylline

A

Methylxanthines - 3rd line
Inhibits phosphodiesterase and blocks adenosine receptors
> increase in cAMP > Increase in activated PKA > Increased phosphorylation of MLCK > Bronchodilation

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8
Q

Montelukast

A

Leukotriene antagonist

Act as antagonists in leukotriene receptors
Decrease in bronchoconstriction, vascular permeability and mucous production

Decrease in eosinophil recruitment

Given orally, preventative for asthma and seasonal allergic rhinitis in patients with asthma

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9
Q

Beclomethasone

A

Corticosteroids

Diffuse into the cytoplasm and bind to receptor then move to nucleus to modify transcription.
Increase anti-inflammatory
Decrease pro-inflammatory mediators

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10
Q

hyoscine butylbromide

A

antispasmodic drug
anticholinergic action exerts a smooth-muscle relaxing/spasmolytic effect
Used in stomach cramps

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11
Q

Propranolol

A

beta-1-adrenergic receptor antagonist used to:
treat high blood pressure
treat conditions that cause an irregular heartbeat (arrhythmia), like atrial fibrillation
help prevent future heart disease, heart attacks and strokes
help prevent chest pain caused by angina

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12
Q

Atenolol

A

Cardioselective beta-1-adrenergic antagonists

Beta blocker medicine, used to treat high blood pressure (hypertension) and irregular heartbeats (arrhythmia).

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13
Q

bisoprolol

A

Beta blocker
beta-1-adrenergic receptor antagonist used to treat high blood pressure (hypertension) and heart failure.

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14
Q

Budesonide

A

Budesonide is a glucocorticoid, which exerts significant local anti-inflammatory effects.

Used for COPD, ulcerative colitis

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15
Q

fluticasone

A

Fluticasone propionate is a glucocorticoid used to treat asthma, inflammatory pruritic dermatoses, and nonallergic rhinitis.

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16
Q

cromoglicate

A

They are used to treat allergic conjunctivitis, a condition triggered by hay fever, house mites and other allergies.
Mast cell stabilisers
Given as eye drops

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17
Q

Bendroflumethiazide

A

Thiazide diuretic

Hypertension

Blocks Na/Cl transporter in distal tubule – mild diuresis

Risk of hypokalaemia due to leaky potassium channels in collecting duct

↑ loss of H+; metabolic alkalosis
↑ loss of K +; Use with K+ -sparing diuretics (see later)
↑ loss of Mg +
↓ loss of uric acid; gout
Erectile dysfunction

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18
Q

Indapamide

A

Thiazide diuretic

Hypertension

Blocks Na/Cl transporter in distal tubule – mild diuresis

↑ loss of H+; metabolic alkalosis
↑ loss of K +; Use with K+ -sparing diuretics (see later)
↑ loss of Mg +
↓ loss of uric acid; gout
Erectile dysfunction

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19
Q

furosemide

A

Loop diuretic

Hypertension

Blocks Na/K/Cl transporter in ascending loop of Henle - Large diuresis

↑ loss of H+; metabolic alkalosis
↑ loss of K +; Use with K+ -sparing diuretics (see later)
↑ loss of Ca +,
↑ loss of Mg +
↓ loss of uric acid; gout

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20
Q

spironolactone

A

Aldosterone antagonist > reduces expression of ENaC and Na/K ATPase in collecting tubule

Little diuresis
Given with other diuretics to limit hypokalaemia

Hyperkalaemia
Gastrointestinal upset
Gynecomastia, menstrual disorders, testicular atrophy (via action on progesterone/androgen receptors outside kidney)

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21
Q

eplerenone

A

Aldosterone antagonist > reduces expression of ENaC and Na/K ATPase in collecting tubule

Little diuresis
Given with other diuretics to limit hypokalaemia

Hyperkalaemia
Gastrointestinal upset
Gynecomastia, menstrual disorders, testicular atrophy (via action on progesterone/androgen receptors outside kidney)

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22
Q

amiloride

A

Epithelial sodium channel blockers

Little diuresis
Given with other diuretics to limit hypokalaemia

Hyperkalaemia
Gastrointestinal upset

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23
Q

triamterene

A

Epithelial sodium channel blockers

Little diuresis
Given with other diuretics to limit hypokalaemia

Hyperkalaemia
Gastrointestinal upset

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24
Q

amlodipine

A

Calcium channel antagonists - Vascular selective

vasodilation

Headache
Flushing - varies with different formulations
Dizziness
Peripheral oedema
↑ gastro-oesophageal reflux

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25
Q

nifedipine

A

Calcium channel antagonists - Vascular selective

vasodilation

Headache
Flushing - varies with different formulations
Dizziness
Peripheral oedema
↑ gastro-oesophageal reflux

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26
Q

ramipril

A

Angiotensin converting enzyme Inhibitor

Hypertension, Heart failure, After MI
Particularly beneficial in patients with higher renin levels

Inhibits angiotensin II synthesis from angiotensin I and therefore inhibiting vasoconstriction and salt retention

Cough
Hypotension
Reversible renal impairment
Hyperkalaemia

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27
Q

lisinopril

A

Angiotensin converting enzyme Inhibitor

Hypertension, Heart failure, After MI
Particularly beneficial in patients with higher renin levels

Inhibits angiotensin II synthesis from angiotensin I and therefore inhibiting vasoconstriction and salt retention

Cough
Hypotension
Reversible renal impairment
Hyperkalaemia

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28
Q

Candesartan

A

Angiotensin II receptor antagonist

Hypertension
Heart failure

Blocks AT receptors on smooth muscle cells -
linked to Gq and then to contraction (inhibits)

Hypotension
Reversible renal impairment
Hyperkalaemia

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29
Q

losartan

A

Angiotensin II receptor antagonist

Hypertension
Heart failure

Blocks AT receptors on smooth muscle cells -
linked to Gq and then to contraction (inhibits)

Hypotension
Reversible renal impairment
Hyperkalaemia

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30
Q

Valsartan

A

Angiotensin II receptor antagonist

Hypertension
Heart failure

Blocks AT receptors on smooth muscle cells -
linked to Gq and then to contraction (inhibits)

Hypotension
Reversible renal impairment
Hyperkalaemia

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31
Q

doxazosin

A

α1-antagonist

hypertension, congestive heart failure, benign prostatic hyperplasia

α1-receptor activation
> activation of Gq,
Activation of PLC (phospholipase C)
↑IP3
↑Ca2+
contraction

Antagonists block this > vasodilation

First dose effect  postural hypotension and syncope

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32
Q

bumetanide

A

Loop diuretic

Heart failure and oedema

Blocks Na/K/Cl transporter in ascending loop of Henle - Large diuresis

↑ loss of H+; metabolic alkalosis
↑ loss of K +; Use with K+ -sparing diuretics (see later)
↑ loss of Ca +,
↑ loss of Mg +
↓ loss of uric acid; gout

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33
Q

minoxidil

A

Potassium channel opener

Severe hypertension, hypertension resistant to other drugs

Activation of ATP-dependent potassium channels
Hyperpolarisation
Closes calcium channels
Less calcium influx
Less contraction

Fluid and salt retention - given with a diuretic to avoid this
Baroreceptor-mediated activation of sympathetic nervous system (increased heart rate and contractility) - given with a beta blocker to avoid this
Given with an inhibitor of RAAS to prevent remodelling effects on the heart.
hypertrichosis (excessive hair growth)

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34
Q

glyceryl trinitrate

A

Organic nitrate

Anti angina; 30 min duration of action

Produce nitric oxide (NO) in endothelial cells
NO diffuses into smooth muscle cell,
activates guanylyl cyclase (GC)
produces cGMP from GTP
relaxation of smooth muscle (vascular, biliary and oesophageal).

More effect on veins than on resistance arteries
 ↓ preload  ↓left and right ventricular chamber size  ↓ wall stress  ↓ oxygen demand – advantage for angina
Has marked effect on larger arteries
 ↓ afterload
↑ coronary vasodilation  ↑ coronary flow
Diverts blood from normal to ischaemic areas of myocardium
Tolerance occurs

Headache
Postural hypotension

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35
Q

Isosorbide mononitrate

A

Organic nitrate

Anti angina; longer duration of action > Twice daily for prophylaxis

Produce nitric oxide (NO) in endothelial cells
NO diffuses into smooth muscle cell,
activates guanylyl cyclase (GC)
produces cGMP from GTP
relaxation of smooth muscle (vascular, biliary and oesophageal).

More effect on veins than on resistance arteries
 ↓ preload  ↓left and right ventricular chamber size  ↓ wall stress  ↓ oxygen demand – advantage for angina
Has marked effect on larger arteries
 ↓ afterload
↑ coronary vasodilation  ↑ coronary flow
Diverts blood from normal to ischaemic areas of myocardium
Tolerance occurs

Headache
Postural hypotension

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36
Q

Nicorandil

A

potassium channel opener and NO donor

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37
Q

Ivabradine

A

slows the heart rate by direct action on the pacemaker in the SA node

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38
Q

colestyramine

A

Bile acid binding resin

dyslipidaemia

Cholesterol is converted to bile acids in liver then secreted in bile
Bile acid binding resins sequester the bile acid and it is excreted in faeces rather than being returned to liver

Constipation
Reduced absorption of other medicines
Fat-soluble vitamin deficiency
Increased triglyceride levels

Avoid in bowel or biliary obstruction

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39
Q

colestipol

A

Bile acid binding resin

dyslipidaemia

Cholesterol is converted to bile acids in liver then secreted in bile
Bile acid binding resins sequester the bile acid and it is excreted in faeces rather than being returned to liver

Decrease in cholesterol in hepatocytes > increased LDL receptor > More LDL removed from circulation

Constipation
Reduced absorption of other medicines
Fat-soluble vitamin deficiency
Increased triglyceride levels

Avoid in bowel or biliary obstruction

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40
Q

Ezetimibe

A

Blocks transport protein NPC1L1 in brush border of enterocytes
Inhibits transport of both dietary and biliary cholesterol

Decrease in cholesterol absorbed > increased LDL receptor > More LDL removed from circulation

GI disturbance
Headache
Hepato-biliary disorders (rare)
Increased risk of rhabdomyolysis if used with a statin

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41
Q

fenofibrate

A

Fibrate - Agonists at PPARα receptor

Increase expression of lipoprotein lipase in muscle
increase fatty acid uptake and oxidation in muscle cells
Decrease triglycerides
Increase apoAI, apoAII synthesis in hepatocytes
 increase plasma HDL

GI side-effects most common
Myositis-like syndrome
Rhabdomyolysis (with statin)

Avoid: hepato-biliary disorders

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42
Q

simvastatin

A

Inhibit HMG-CoA reductase - Responsible for converting HMG-CoA to mevalonate

> Inhibits synthesis of cholesterol in liver > increased LDL receptor/decreased lipoprotein synthesis > More LDL removed from circulation

ADRs
GI disturbances, insomnia, rashes
Hepato-biliary effects
Monitor LFT’s (baseline, within 3 months and at 12 months)
Transaminases
Myopathy / rhabdomyolysis
Advise patients to seek medical advice if develop muscle pain, tenderness or weakness

Contra-indications
Active liver disease
Pregnancy, breast-feeding

CP450 interactions:
Avoid -
Antibacterials (Clarithromycin, erythromycin)
Antifungals (Azoles – ketoconazole, itraconazole)
Grapefruit juice

Do not exceed simvastatin 20mg/day
Amiodarone
Anticoagulants
Calcium-channel blockers
Amlodipine
Diltiazem
Verapamil
10mg/day
Fibrates (bezafibrate or ciprofibrate)

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43
Q

Atorvastatin

A

Inhibit HMG-CoA reductase - Responsible for converting HMG-CoA to mevalonate

> Inhibits synthesis of cholesterol in liver > increased LDL receptor/decreased lipoprotein synthesis > More LDL removed from circulation

ADRs
GI disturbances, insomnia, rashes
Hepato-biliary effects
Monitor LFT’s (baseline, within 3 months and at 12 months)
Transaminases
Myopathy / rhabdomyolysis
Advise patients to seek medical advice if develop muscle pain, tenderness or weakness

Contra-indications
Active liver disease
Pregnancy, breast-feeding

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44
Q

pravastatin

A

Inhibit HMG-CoA reductase - Responsible for converting HMG-CoA to mevalonate

> Inhibits synthesis of cholesterol in liver > increased LDL receptor/decreased lipoprotein synthesis > More LDL removed from circulation

ADRs
GI disturbances, insomnia, rashes
Hepato-biliary effects
Monitor LFT’s (baseline, within 3 months and at 12 months)
Transaminases
Myopathy / rhabdomyolysis
Advise patients to seek medical advice if develop muscle pain, tenderness or weakness

Contra-indications
Active liver disease
Pregnancy, breast-feeding

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45
Q

alirocumab

A

monoclonal antibody for PCSK9

PCSK9 normally decreases LDL receptor number
Alirocumab ↑LDL receptors
Given s.c. every 2 weeks.
Use when statin or statin/ezetimibe are not sufficiently effective

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46
Q

Amiodarone

A

Class III antiarrhythmic
Multiple mechanisms – all include prolongation of the action potential and reduction of abnormal automaticity. (poss block of delayed rectifier potassium channel)

Both supraventricular and ventricular arrhythmias

Hypotension, photosensitivity, pulmonary fibrosis
Some ADRs related to its structural similarity to thyroid hormone

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47
Q

dronedarone

A

Class III antiarrhythmic
Multiple mechanisms – all include prolongation of the action potential and reduction of abnormal automaticity. (poss block of delayed rectifier potassium channel)

Atrial fibrillation and flutter

Fewer ADRs than amiodarone but also less effective
Diarrhoea, nausea, vomiting.

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48
Q

sotalol

A

Class III antiarrhythmic - also has beta-blocking effects

Multiple mechanisms – all include prolongation of the action potential and reduction of abnormal automaticity. (poss block of delayed rectifier potassium channel)

Both supraventricular and ventricular arrhythmias

Torsades de pointes
bronchospasm

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49
Q

lidocaine

A

Class IB antiarrhythmic
Sodium channel blocker

fast association and dissociation  prevents premature beat - blocks when cells are depolarised.

Ventricular arrhythmias

Seizures
Nystagmus

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50
Q

flecainide

A

Class IC antiarrhythmic
Sodium channel blocker

slows rate of depolarization

Atrial fibrillation, Ventricular arrhythmias, Ventricular tachycardia, Certain congenital ventricular arrhythmias

Blurred vision, Exacerbate congestive heart failure, Exacerbate some arrhythmias, Overall mortality increased after MI

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51
Q

disopyramide

A

Class IA antiarrhythmic
Sodium channel blocker

slows rate of depolarization

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52
Q

Diltiazem

A

Class IV L-type Calcium channel blockers – cardio selective

Slow conduction in SA and AV nodes
Shorten plateau of action potential and reduce force of contraction
Decreased calcium entry  decrease after-depolarisation.

Supraventricular arrhythmias

Worsening of heart failure
Constipation
Sinus bradycardia or AV block
(do not use with beta blockers)

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53
Q

verapamil

A

Class IV L-type Calcium channel blockers – cardio selective

Slow conduction in SA and AV nodes
Shorten plateau of action potential and reduce force of contraction
Decreased calcium entry  decrease after-depolarisation.

Supraventricular arrhythmias

Worsening of heart failure
Constipation
Sinus bradycardia or AV block
(do not use with beta blockers)

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54
Q

Adenosine

A

Unclassified antiarrhythmic

Activates A1 adenosine receptors in AV node
activate inward rectifier potassium channel
hyperpolarisation, slows rate of rise of pacemaker
i.v. lasts 20-30s
terminates supraventricular tachycardias

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55
Q

One example of how drugs can induce arrhythmias

A

The hERG channel was identified in the 1990s and shown to be the channel responsible for one of the repolarising potassium currents IKR.
Block of the hERG channel slows repolarisation and leads to “long QT syndrome”.

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56
Q

Aspirin

A

Inhibits COX-1 irreversibly and hence TxA2 production by platelets
Also inhibits prostacyclin synthesis (reversibly) in vascular endothelium

Secondary prevention of MI
Management of cerebrovascular disease
Prevention of vascular events in pts with peripheral vascular disease (PVD)

Bleeding – approx 1 in 200 pts
GI intolerance
Hypersensitivity
0.2% general population
4% of asthmatics
Risk of Reyes syndrome in children - avoid

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57
Q

clopidogrel

A

P2Y (ADP) receptor antagonists

Irreversibly blocks effect of ADP on platelets

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58
Q

prasugrel

A

P2Y (ADP) receptor antagonists - anti-platelet

Irreversibly blocks effect of ADP on platelets

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59
Q

abciximab

A

GPIIb/IIIa inhibitors - anti-platelet

Limited to single use

Blocks binding of fibrinogen
Prevents platelet aggregation

given iv; adjunct to aspirin and heparin for coronary artery angioplasty, stenting

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60
Q

alteplase

A

Fibrinolytic

human recombinant t-PA,
activates plasminogen bound to fibrin
longer half life

Acute ischaemic stroke
Arterial thrombosis
Life threatening venous thrombosis
Acute MI (given within 12 h)

ADRs:
Bleeding
Allergic reactions (streptokinase more antigenic, recombinant are less antigenic)

Contraindications:
Internal bleeding
Pregnancy
Trauma (incl CPR)

Tranexamic acid inhibits fibrinolysis

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61
Q

streptokinase

A

Fibrinolytic - directly converts plasminogen to active plasmin

Acute ischaemic stroke
Arterial thrombosis
Life threatening venous thrombosis
Acute MI (given within 12 h)

ADRs:
Bleeding
Allergic reactions (streptokinase more antigenic, recombinant are less antigenic)

Contraindications:
Internal bleeding
Pregnancy
Trauma (incl CPR)

Tranexamic acid inhibits fibrinolysis

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62
Q

enoxaparin

A

Low molecular weight heparins

Subcutaneous
Preferred over heparin (longer acting, longer half life)
Inhibit Xa (but not thrombin)
Monitoring not required
Not neutralised by protamine

Thromboprophylaxis (low doses)
DVT and PE – prevents extension of thrombosis
Prevent coronary events e.g. in unstable angina
MI – prevents extension of thrombosis

Haemorrhage
Heparin-induced thrombocytopenia
Osteoporsis
Hyperkalaemia

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63
Q

dalteparin

A

Low molecular weight heparins

Subcutaneous
Preferred over heparin (longer acting, longer half life)
Inhibit Xa (but not thrombin)
Monitoring not required
Not neutralised by protamine

Thromboprophylaxis (low doses)
DVT and PE – prevents extension of thrombosis
Prevent coronary events e.g. in unstable angina
MI – prevents extension of thrombosis

Haemorrhage
Heparin-induced thrombocytopenia
Osteoporsis
Hyperkalaemia

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64
Q

edoxaban

A

Orally-active Xa inhibitor (DOAC)

No reversal agent

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65
Q

rivaroxaban

A

Orally-active Xa inhibitor

Reversed by andexanet alfa

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66
Q

warfarin

A

Given orally
Inhibits factors VII, IX, X, II
4-5 days for full effect
Reversed by giving vitamin K
Vitamin K occurs in green vegetables and green tea
Requires monitoring – prothrombin time measured and expressed as INR (International Normalised Ratio) of 2 - 4.
Metabolised by CYP2C9 – half life variable

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67
Q

Epoprostenol

A

= prostacyclin, PGI2
Bind to prostacyclin IP receptors
Increase platelet cAMP
Inhibits platelet aggregation and adhesion. Vasodilation.
ADRs: flushing headache and hypotension
IV, short-lived
Used in haemodialysis, severe pulmonary hypertension and circulatory shock associated with meningococcal septicaemia

68
Q

Dipyridamole

A

Phosphodiesterase inhibitor ↑cAMP levels
Inhibits cellular reuptake of adenosine:
↑ plasma [adenosine]
→ activates A2 receptors
→ ↑ adenylyl cyclase, cAMP
→ inhibit expression of cell surface GPIIb/IIIa receptors

Licensed for prophylaxis of thromboembolism associated with prosthetic heart valves (with warfarin)
ADRs:
Hypotension,
can exacerbate migraine
Angina pectoris

69
Q

Heparin

A

Family of sulphated glycosaminoglycans present in mast cells.
Activates antithrombin III which inhibits thrombin, factor X and other serine proteases (II, IX, XI, XII)
Short-acting, half life depends on dose administered
Given by injection
Monitoring with APTT test (activated partial thromboplastin time)
Antidote = protamine

70
Q

Sacubitril

A

Neprolysin inhibitors

In heart failure, natriuretic peptides (BNP and NT-pro BNP) are elevated and reduce disease progression.
Sacubitril inhibits neprilysin which breaks down natriuretic peptides, bradykinin and angiotensin II.
It is combined with valsartan (an ARB) to prevent the effects of raised angiotensin II (known as ARNIs).

71
Q

Digoxin

A

binds to potassium binding site of Na+/K+ ATPase and inhibits.
↓ sodium gradient.
The Na+/Ca2+ exchanger needs this gradient to move Ca2+ out of the cell.
↑ calcium in cell
↑ force of contraction (for heart failure)

Digoxin has a very low therapeutic index
ectopic beats
induce ventricular tachycardia and ventricular fibrillation
nausea, vomiting,
diarrhoea
confusion

Digoxin and K+ compete for binding to the Na+/K+ ATPase so if K levels are low as in hypokalaemia, the effect of digoxin is increased – dangerous!
It tends to be used when patients have not responded sufficiently to diuretics and ACE-I

For arrhythmias, Slowed conduction through AV node
Increasing the refractory period of the AV node reduces ventricular rate.
Used to slow ventricular rate in rapid persistent atrial fibrillation.

72
Q

milrinone

A

Increased contractility E.g. milrinone
Inhibition of phosphodiesterase leads to increased levels of cAMP
 increased force of contraction
But also increased potential for dysrhythmias

73
Q

Dabigatran etexilate

A

Thrombin inhibitor
Pro-drug
Rapid onset

74
Q

Paracetamol

A

analgesic and antipyretic but NOT anti-inflammatory

Action likely in CNS

few gastric or platelet side effects at therapeutic doses
not really a NSAID

Overdose  potentially fatal hepatic necrosis through conversion to a toxic metabolite NAPQI and subsequent depletion of glutathione  oxidative stress and damage.
Treatment of overdose:
Activated charcoal within 4 hours if dose > 7.5 g
N-acetylcysteine – acts as glutathione substitute and detoxifies NAPQI
Liver failure  transplant

75
Q

Ibuprofen

A

Most common choice of NSAID for mild-moderate pain

COX inhibitor

inhibition of: Vasodilation, effects of histamine and bradykinin on vascular permeability, hyperalgesia, Regulation of temperature set point

ADRs: ↓ mucus and bicarbonate secretion, ↑ acid secretion, Nephrotoxicity, skin rashes, cardovascular effects.

Short half-life, Low solubility in water  preparation for iv is difficult, Insoluble in the stomach  slow and erratic absorption, Controlled release formulations using liposomes, polymers or nanoparticles  release in intestine or even colon  plasma concentrations are very low

76
Q

Diflofenac

A

NSAID: Cox inhibitor

inhibition of: Vasodilation, effects of histamine and bradykinin on vascular permeability, hyperalgesia, Regulation of temperature set point

ADRs: ↓ mucus and bicarbonate secretion, ↑ acid secretion, Nephrotoxicity, skin rashes, cardovascular effects.

77
Q

etoricoxib

A

NSAID: Cox 2 inhibitor

inhibition of: Vasodilation, effects of histamine and bradykinin on vascular permeability, hyperalgesia, Regulation of temperature set point

ADRs: ↓ mucus and bicarbonate secretion, ↑ acid secretion, Nephrotoxicity, skin rashes, cardovascular effects.

78
Q

Naproxen

A

NSAID: Cox inhibitor

inhibition of: Vasodilation, effects of histamine and bradykinin on vascular permeability, hyperalgesia, Regulation of temperature set point

ADRs: ↓ mucus and bicarbonate secretion, ↑ acid secretion, Nephrotoxicity, skin rashes, cardovascular effects.

79
Q

codeine

A

Analgesic action via µ opioid receptors.

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

metabolised to the more potent morphine

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

80
Q

Morphine

A

Analgesic action via µ opioid receptors.

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

81
Q

tramadol

A

Dual action
Opioid receptor agonist
Noradrenaline and 5HT reuptake inhibition

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

Only partially reversed by naloxone (opioid antagonist)
Metabolised in liver  Active metabolite
? less constipation & respiratory depression
Caution in epilepsy, renal/hepatic impairment, & with drugs that can lower the seizure threshold

82
Q

pethidine

A

Analgesic action via µ opioid receptors.

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

83
Q

Fentanyl

A

Analgesic action via µ opioid receptors. also at delta and kappa opioid receptors

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

84
Q

Methadone

A

Analgesic action via µ opioid receptors.

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

85
Q

Oxycodone

A

Analgesic action via µ opioid receptors. also at delta and kappa opioid receptors

Useful for acute pain and “end of life” pain but not neuropathic or chronic pain

GPCRs – coupled to Gi
decreased cAMP and increased potassium conductance
hyperpolarisation
decreased neurotransmitter release

ADRs: constipation, sedation, nausea etc

86
Q

Naloxone

A

Opioid antagonist

reverses effects of opioid overdose

87
Q

cyclizine

A

Histamine antagonists in nausea and vomiting
Act on H1 histamine receptors in CNS
Also have some antimuscarinic actions
Used particularly for motion sickness, vestibular disorders, nausea and vomiting associated with surgery
Unwanted effects: sedation, drowsiness, dry mouth, constipation, urinary retention, blurred vision

88
Q

promethazine dont need to know

A

Histamine antagonists in nausea and vomiting
Act on H1 histamine receptors in CNS
Also have some antimuscarinic actions
Used particularly for motion sickness, vestibular disorders, nausea and vomiting associated with surgery
Unwanted effects: sedation, drowsiness, dry mouth, constipation, urinary retention, blurred vision

89
Q

cinnarizine dont need to know

A

Histamine antagonists in nausea and vomiting
Act on H1 histamine receptors in CNS
Also have some antimuscarinic actions
Used particularly for motion sickness, vestibular disorders, nausea and vomiting associated with surgery
Unwanted effects: sedation, drowsiness, dry mouth, constipation, urinary retention, blurred vision

90
Q

hyoscine

A

Muscarinic antagonists in nausea and vomiting
Used particularly for motion sickness, vestibular disorders, nausea and vomiting associated with surgery
Oral or transdermal patch
Unwanted effects: constipation; dizziness; drowsiness; dry mouth; dyspepsia; flushing; headache; palpitations; skin reactions; tachycardia; urinary disorders; vision disorders.

91
Q

domperidone

A

Dopamine antagonists in nausea and vomiting
SPECIFICALLY ONLY THE PERIPHERY
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

92
Q

metoclopramide

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

93
Q

chlorpromazine dont need to know

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

94
Q

haloperidol

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8 - High dopamine associated with delusions
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

95
Q

droperidol dont need to know

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

96
Q

prochlorperazine dont need to know

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

97
Q

trifluoperazine dont need to know

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

98
Q

levomepromazine dont need to know

A

Dopamine antagonists in nausea and vomiting
Act as antagonists at D2 dopamine receptors in the chemoreceptor trigger zone (also act on histamine H1 and muscarinic receptors elsewhere).
Administration: oral, iv, suppository.
Used for severe nausea and vomiting associated with cancer, radiation sickness, cytotoxic drugs, post-operative nausea
These are all antipsychotics (except for domperidone)  module 8
Unwanted effects: sedative, hypotension, menstrual cycle irregularities, movement disorders, parkinsonism, diarrhoea.

99
Q

ondansetron

A

Serotonin antagonists in nausea and vomiting
Antagonists at 5HT3 receptors in gastrointestinal tract and CNS including the chemoreceptor trigger zone.
5HT is released from enterochromaffin cells in the gut then activates 5HT3 receptors on vagal sensory fibres.
Irritants can also activate sensory fibres in the gut
Used for nausea and vomiting associated with chemotherapy and radiotherapy, post-operative nausea and vomiting.
Administration: transdermal, IV, oral
Unwanted effects: constipation, feeling hot, headache.

100
Q

granisetron dont need to know

A

Antagonists at 5HT3 receptors in gastrointestinal tract and CNS including the chemoreceptor trigger zone.
5HT is released from enterochromaffin cells in the gut then activates 5HT3 receptors on vagal sensory fibres.
Irritants can also activate sensory fibres in the gut
Used for nausea and vomiting associated with chemotherapy and radiotherapy, post-operative nausea and vomiting.
Administration: transdermal, IV, oral
Unwanted effects: constipation, feeling hot, headache.

101
Q

Ispagula husk dont need to know

A

Bulk laxative
Indigestible polysaccharides
Increased volume of intestinal contents stimulates stretch receptors and peristalsis
May take several days to work
No serious unwanted effects (possibly some bloating)

102
Q

Macrogol

A

Osmotic Laxatives
Are not absorbed and trap fluid in the lumen
Must have sufficient fluid intake
Can take 2-3 days to act
Unwanted effects: flatulence, cramps, electrolyte disturbance

103
Q

lactulose

A

Osmotic Laxatives
Are not absorbed and trap fluid in the lumen
Must have sufficient fluid intake
Can take 2-3 days to act
Unwanted effects: flatulence, cramps, electrolyte disturbance

104
Q

docusate dont need to know

A

Faecal Softener
Anionic surfactant – lowers surface tension and allows mixing of aqueous and fatty substances to soften the stool.
Stimulate intestinal fluid and electrolyte secretion

105
Q

bisacodyl

A

Stimulant laxative
Bisacodyl stimulates sensory nerve endings
Senna stimulates myenteric plexus
Use lowest dose and shortest time
Unwanted effects: flatulence, cramps, electrolyte disturbance

106
Q

Senna

A

Stimulant laxative
Bisacodyl stimulates sensory nerve endings
Senna stimulates myenteric plexus
Use lowest dose and shortest time
Unwanted effects: flatulence, cramps, electrolyte disturbance

107
Q

Alginates

A

Alginates form a viscous gel (‘raft’) that floats on the surface of the stomach contents, reducing acid reflux. Usually combined with antacids.

108
Q

Ranitidine

A

Ranitidine is a competitive inhibitor of histamine H2-receptors. The reversible inhibition of H2-receptors in gastric parietal cells results in a reduction in both gastric acid volume and concentration.

109
Q

omeprazole

A

PPI

110
Q

Lansoprazole

A

PPI

111
Q

Acetylcysteine

A

paracetamol overdose

112
Q

Metformin

A

Unclear but likely involves:
• reduced liver glucose
production
• increased glucose uptake and
utilisation in skeletal muscle
• Reduced intestinal
carbohydrate absorption
Most widely prescribed Generally well tolerated and no hypoglycaemia or weight gain

113
Q

Glicazide

A

Act on ATP-dependent potassium ion channels in pancreatic beta cells. Block of these channels results in depolarisation of the beta cell and thus release of insulin.
Can cause hypoglycaemia, weight gain (these effects less pronounced in the non- sulfonylurea type)
Requires beta cells to be functional

114
Q

Sitagliptin

A

Dipeptidylpeptidase 4 (DPP4) is the enzyme that terminates the actions of the incretins GIP and GLP-1 which would normally stimulate insulin secretion, reduce pancreatic glucagon secretion and reduce gastric emptying (so slow rate of nutrient absorption).
Not associated with weight gain and little hypoglycaemia than sulfonylureas.

115
Q

Clomiphene

A

Oestrogen Antagonist SERM

Antagonist in hypothalamus and anterior pituitary gland, partial agonist in the ovaries

Blocks oestrogen receptors in pituitary  relief of negative feedback inhibition  increased release of GnRH and gonadotropins  ↑ FSH  stimulate follicle growth  oestrogen trigger signal  LH surge  ovulation

Induces ovulation

116
Q

ethinylestradiol

A

Oestrogen agonists (analogues)

less first pass metabolism

Replacement therapy:
Primary hypogonadism – stimulate development of secondary sexual characteristics
At or after menopause  prevent menopausal symptoms (flushing, vaginal dryness, protect against osteoporosis)
Contraception

Side effects
tenderness in breasts
endometrial hyperplasia
Risk of thromboembolism
oedema
Migraines, hyperpigmentation, uterine bleeding (postmenopausal)

117
Q

finasteride

A

Inhibitors of the enzyme 5α-reductase prevent the metabolism of testosterone to its active metabolite dihydrotestosterone.

Prostate cells are dependent on androgen stimulation for survival → slows the growth of prostate tissue
Used in:
Benign prostatic hyperplasia
Androgenetic alopecia

118
Q

goserelin

A

GnRH Agonist

Given in pulses (s.c.) to mimic physiological secretion of GnRH, stimulate gonadotrophin release and induce ovulation

It is possible to suppress the hypothalamic-pituitary–gonadal axis either by continuous administration of a GnRH agonist or by administration of a GnRH receptor antagonist

Continuous use, by nasal spray or as depot preparations, transiently stimulates then inhibits gonadotrophin release because of downregulation (desensitisation) of GnRH receptors in the pituitary.

-> cause gonadal suppression, used in:
prostate and breast cancers,
endometriosis
large uterine fibroids.

119
Q

levonorgestrel

A

Progesterone agonist

Active orally

GnRH suppression
Decreases oestrogen stimulated endometrial proliferation
Increased viscosity of cervical mucus
Fat and carbohydrate metabolism
Decrease Na+ reabsorption
Development of breast and endometrium

Used in Contraception
With oestrogen in combined oral contraceptive pill
Progesterone-only pill
Injectable or implantable progesterone-only contraception
Part of intrauterine contraceptive system
HRT – combined with oestrogen
Long-term ovarian suppression (resulting in prolonged anovulation and amenorrhea)*
Endometriosis
Endometrial carcinoma

Side effects
Weak androgenic actions (see next section)
Acne
Fluid retention
Weight change
Depression
Change in libido
Breast discomfort
Irregular menstrual cycles and breakthrough bleeding
Increased risk of thromboembolism

120
Q

medroxyprogesterone acetate

A

Progesterone agonist

Active orally

GnRH suppression
Decreases oestrogen stimulated endometrial proliferation
Increased viscosity of cervical mucus
Fat and carbohydrate metabolism
Decrease Na+ reabsorption
Development of breast and endometrium

Used in Contraception
With oestrogen in combined oral contraceptive pill
Progesterone-only pill
Injectable or implantable progesterone-only contraception
Part of intrauterine contraceptive system
HRT – combined with oestrogen
Long-term ovarian suppression (resulting in prolonged anovulation and amenorrhea)*
Endometriosis
Endometrial carcinoma

Side effects
Weak androgenic actions (see next section)
Acne
Fluid retention
Weight change
Depression
Change in libido
Breast discomfort
Irregular menstrual cycles and breakthrough bleeding
Increased risk of thromboembolism

121
Q

norethisterone

A

Progesterone agonist

Active orally

GnRH suppression
Decreases oestrogen stimulated endometrial proliferation
Increased viscosity of cervical mucus
Fat and carbohydrate metabolism
Decrease Na+ reabsorption
Development of breast and endometrium

Used in Contraception
With oestrogen in combined oral contraceptive pill
Progesterone-only pill
Injectable or implantable progesterone-only contraception
Part of intrauterine contraceptive system
HRT – combined with oestrogen
Long-term ovarian suppression (resulting in prolonged anovulation and amenorrhea)*
Endometriosis
Endometrial carcinoma

Side effects
Weak androgenic actions (see next section)
Acne
Fluid retention
Weight change
Depression
Change in libido
Breast discomfort
Irregular menstrual cycles and breakthrough bleeding
Increased risk of thromboembolism

122
Q

desogestrel

A

Progesterone agonist

Active orally

GnRH suppression
Decreases oestrogen stimulated endometrial proliferation
Increased viscosity of cervical mucus
Fat and carbohydrate metabolism
Decrease Na+ reabsorption
Development of breast and endometrium

Used in Contraception
With oestrogen in combined oral contraceptive pill
Progesterone-only pill
Injectable or implantable progesterone-only contraception
Part of intrauterine contraceptive system
HRT – combined with oestrogen
Long-term ovarian suppression (resulting in prolonged anovulation and amenorrhea)*
Endometriosis
Endometrial carcinoma

Side effects
Weak androgenic actions (see next section)
Acne
Fluid retention
Weight change
Depression
Change in libido
Breast discomfort
Irregular menstrual cycles and breakthrough bleeding
Increased risk of thromboembolism

123
Q

raloxifene

A

SERM: selective oestrogen receptor modulators

Antagonist used to ↓ breast cancer
Partial agonist - Used for treatment of osteoporosis

124
Q

Tamoxifen

A

SERM: selective oestrogen receptor modulators

Antagonist used to ↓ breast cancer
Agonist at bone
Agonist at endometrium - cancer

125
Q

Tamsulosin

A

Tamsulosin is a type of medicine known as an alpha blocker (or alpha-adrenoreceptor antagonist).

If you have an enlarged prostate gland it helps by relaxing the muscle around the bladder and prostate gland, making it easier to pee.

In some cases it can also be used to help ease the passing of kidney stones through the urinary tract.

126
Q

anastrozole

A

Aromatase inhibitor

127
Q

phenytoin

A
  • use-dependent block of sodium channels
  • reduces repetitive firing of action potentials
  • used for tonic-clonic seizures
128
Q

valproate

A
  • block of sodium channels  reduces repetitive firing of action potentials
  • and block of T-type calcium channels  decreases rhythmic discharge of thalamic neurons associated with absence seizures
  • and inhibits GABA transaminase so raises GABA levels  increases levels of inhibition.
  • Used for absent and tonic clonic seizures
129
Q

carbamazepine

A
  • use-dependent block of sodium channels
  • reduces repetitive firing of action potentials
  • used for tonic-clonic seizures and partial seizures. Also used for neuropathic pain and manic-depressive illness.
130
Q

ethosuximide

A

Calcium channel block
Used for absence seizures (may exacerbate tonic-clonic seizures)

131
Q

diazepam

A

Benzodiazepine agonists
Act quickly so good for emergency use – buccal, rectal or iv
Increases GABA inhibitory effect
AE:
Tolerance and dependence  withdrawal syndrome which can exacerbate seizures if stopped abruptly. Not good for long-term treatment
Sedative

132
Q

midazolam

A

Benzodiazepine agonists
Act quickly so good for emergency use – buccal, rectal or iv
Increases GABA inhibitory effect
AE:
Tolerance and dependence  withdrawal syndrome which can exacerbate seizures if stopped abruptly. Not good for long-term treatment
Sedative

133
Q

lorazepam

A

Benzodiazepine agonists
Act quickly so good for emergency use – buccal, rectal or iv
Increases GABA inhibitory effect
AE:
Tolerance and dependence -> withdrawal syndrome which can exacerbate seizures if stopped abruptly. Not good for long-term treatment
Sedative

134
Q

Clonazepam

A

Benzodiazepine agonists
Act quickly so good for emergency use – buccal, rectal or iv
Increases GABA inhibitory effect
AE:
Tolerance and dependence  withdrawal syndrome which can exacerbate seizures if stopped abruptly. Not good for long-term treatment
Sedative

135
Q

Tiagabine (not on drug list)

A
  • inhibits GAT = GABA transporter.
    used as add-on therapy for partial seizures
    Drowsiness, confusion, dizziness
136
Q

Vigabatrin (not on drug list)

A

Irreversibly inhibit GABA transaminase, ↓ GABA breakdown
Designer drug
Restricted to patients with resistant epilepsy

Irreversible peripheral visual field defects -> systematic screening

137
Q

Temazepam

A

Benzodiazepine agonists
Act quickly so good for emergency use – buccal, rectal or iv
Increases GABA inhibitory effect
AE:
Tolerance and dependence  withdrawal syndrome which can exacerbate seizures if stopped abruptly. Not good for long-term treatment
Sedative

138
Q

L-DOPA

A

Replaces lost dopamine in parkinson’s disease
Improves tremor, rigidity, bradykinesia

adverse effects:
Nausea and anorexia (treat with domperidone* (DA antagonist in periphery) or cyclizine (anti-histamine))
Hypotension
Dyskinesias (involuntary movements)
Hallucinations, psychosis and confusion (Treat with non-dopaminergic antipsychotics! E.g. clozapine, quetiapine)
Also impulse control disorders
Increased risk of suicide

139
Q

carbidopa

A

Inhibits DOPA decarboxylase so reduces conversion to noradrenaline in peripheral nervous system.

When given with L-DOPA: co-careldopa

140
Q

co-careldopa

A

L-DOPA + Carbidopa
Replaces lost dopamine in parkinson’s disease
Improves tremor, rigidity, bradykinesia

Inhibits DOPA decarboxylase so reduces conversion to noradrenaline in peripheral nervous system.

141
Q

entacapone

A

Catechol-O-methyltransferase (COMT) inhibitor
Prevents L-DOPA breakdown in periphery so more gets to brain

142
Q

selegiline

A

Monoamine oxidase B inhibitor
Prevents dopamine breakdown

143
Q

ropinirole

A

Dopamine agonists
ADRs: Drowsy, hallucinations, compulsive disorders

144
Q

rivastigmine

A

Reversible cholinesterase inhibitor
Selective (relatively) for CNS
First-line for mild-moderate AD and vascular dementia
6-12 month delay in progression
Caution: bradycardia
Unwanted effects:
GI distress – muscle cramping
Abnormal dreams

145
Q

donepezil

A

Reversible cholinesterase inhibitor
Selective (relatively) for CNS
First-line for mild-moderate AD and vascular dementia
6-12 month delay in progression
Caution: bradycardia
Unwanted effects:
GI distress – muscle cramping
Abnormal dreams

146
Q

memantine

A

NMDA antagonist – non-competitive
Prevents glutamate-induced excitotoxicity but doesn’t interfere with learning and memory
Used in moderate to severe dementia

147
Q

amitriptyline

A

Tricyclic Antidepressants
e.g. amitriptyline, imipramine
a.k.a. SNRIs : block both NA and 5HT reuptake
Also have antimuscarinic activity and antihistamine activity
Dangerous in overdose and when taken with alcohol.

Unwanted effects:
Dry mouth, constipation, blurred vision, urinary retention, sedation, confusion, postural hypotension, impotence, seizures.
Can cause prolonged QT  sudden cardiac death (quinidine-like)

148
Q

fluoxetine

A

SSRIs
e.g. fluoxetine, citalopram, sertraline
Unwanted effects: nausea, diarrhoea, insomnia
Low risk of overdose
Do not use in combination with MAO inhibitors
Can inhibit metabolism of other drugs.
Not recommended in children
Can get prolonged QT  sudden cardiac death

149
Q

citalopram

A

SSRIs
e.g. fluoxetine, citalopram, sertraline
Unwanted effects: nausea, diarrhoea, insomnia
Low risk of overdose
Do not use in combination with MAO inhibitors
Can inhibit metabolism of other drugs.
Not recommended in children
Can get prolonged QT  sudden cardiac death

150
Q

sertraline

A

SSRIs
e.g. fluoxetine, citalopram, sertraline
Unwanted effects: nausea, diarrhoea, insomnia
Low risk of overdose
Do not use in combination with MAO inhibitors
Can inhibit metabolism of other drugs.
Not recommended in children
Can get prolonged QT  sudden cardiac death

151
Q

lofepramine

A

NRIs
e.g. lofepramine
Unwanted effects: headache, dry mouth, insomnia
Used in depression associated with anxiety.

152
Q

venlafaxine

A

SNRIs
e.g. venlafaxine, duloxetine,
Unwanted effects: sedation, dizziness
Low risk of overdose
Do not use in combination with MAO inhibitors

Note: St John’s wort
Few reported side effects
Can inhibit metabolism of other drugs.

153
Q

mirtazapine

A

Monoamine receptor antagonists.
Mirtazepine = α2 and 5HT2c (and histamine) presynaptic inhibitory receptor antagonist => increase NA and 5HT release

154
Q

Zopiclone

A

Z-drugs, e.g. zopiclone and zolpidem
Act at benzodiazepine receptors but do not have a benzodiazepine chemical structure
Subtype selective for α1 subunit containing receptors
Used for sleep and axiety issues

155
Q

Chlorpromazine

A

sedating antipsychotic
Reduced aggressiveness, agitation and delusion in schizophrenic patients
Produced a characteristic akinesia
called “major tranquillizer” or “neuroleptic”
Show
Show “extra-pyramidal” side-effects = acute dystonia and tardive dyskinesia

156
Q

olanzepine

A

Dopamine antagonist
Second-generation anti-psychotics a.k.a “atypical”
e.g. clozapine, risperidone, olanzepine, quetiapine
Fewer extra-pyramidal side effects

157
Q

quetiapine

A

Dopamine antagonist
Second-generation anti-psychotics a.k.a “atypical”
e.g. clozapine, risperidone, olanzepine, quetiapine
Fewer extra-pyramidal side effects

158
Q

Lithium

A

Unclear MoA
Used for long term bipolar treatment

159
Q

cyclophosphamide

A

Alkylating agent
chemically reactive and form covalent bonds with guanine or adenine nucleotides.
inhibit replication and transcription by binding directly to DNA

160
Q

doxorubicin

A

forms DNA adduct, inhibits topoisomerase (needed for uncoiling DNA), promotes free radical formation - prevent DNA repair
Cardiotoxicity

161
Q

methotrexate

A

Methotrexate is an analogue of folic acid
Inhibits dihydrofolate reductase (DHFR)

162
Q

5-fluorouracil

A

inhibits thymidylate synthase
Needed for nucleotide synthesis

163
Q

Cisplatin`

A

forms a complex with the nitrogen atoms in guanines
inhibit replication and transcription
single- and double-stranded breaks and miscoding
 can induce apoptosis.

164
Q

vincristine

A

Inhibit appropriate assembly of microtubules
Cells blocked in mitosis

165
Q

Paclitaxel

A

Inhibit appropriate disassembly of microtubules
Cells blocked in mitosis

166
Q

Aciclovir

A

nucleotide analogue

GEM (18 decks)

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