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Flashcards in Pharmacology Deck (453):
1

What is the group of drugs used to treat myasthenia gravis?

Muscle excitors

2

Name the two drugs used to treat myasthenia gravis

Edrophonium/ Tensilon
Pyridostigmine

3

What is the pharmacological name for tensilon?

Edrophonium

4

What is the trivial/ brand name for edrophonium?

Tensilon

5

What is tensilon?

Muscle excitor used to treat myasthenia gravis

6

How does tensilon work?

Competitively inhibits acetyl-cholinesterase, preventing breakdown of Ach. In MG will greatly increase muscle function.

7

Why can tensilon act as a test for MG?

It's a temporary drug which will improve muscle function in MG but make other syndromes worse.

8

How does pyridostigmine work against MG?

Inhibits the hydrolysis of Ach by competitively inhibiting acetyl-cholinesterase. Results in the increase of Ach.

9

What class of drug is pyridostigmine?

Reversible cholinesterase inhibitor

10

What class of drug is tensilon/ endrophonium?

Cholinesterase inhibitor

11

Name the main drugs that act as muscle relaxants

Tubocurarine
Suxamethonium
Atracurium

12

How does Tubocurarine work?

Blocks the receptor site for Ach
Also causes histamine release.

13

How does Suxamethonium work?

Depolarises post synaptic membrane so muscle can't contract.

14

How does Atracurium work?

Antagonises neurotransmitter action of Ach by competitively binding with cholinergic receptor sites on the motor end-plate.

15

What is Suxamethonium clinically used for?

Induced muscle relaxation/short term paralysis for tracheal intubation

16

What is Atracurium clinically used for?

Used adjunctively in tracheal intubation to provide skeletal muscle relaxation.

17

What is Tubocurarine clinically used for?

Used as a poison and spider bite antidote.

18

What receptors do Tubocurarine, Suxamethonium and Atracurium all mutually act on?

Cholinergic receptors

19

Which of these drugs is a cholinergic agonist?
Tubocurarine
Suxamethonium
Atracurium

Suxamethonium

20

What is the are the differences between Suxamethonium and Atracurium as nicotinic cholinergic drugs?

Suxamethonium - Depolarising Agonist
Atracurium - Non-depolarising Anatagonist

21

Why is Tropicamide commonly used for lens and retina examinations?

Clinically reduces eye movement

22

Name two muscarinic cholinergic receptor agonists

Muscarine
Pilocarpine

23

How do muscarinic cholinergic receptor agonists work?

Mimics action of the neurotransmitter acetylcholine by binding muscarinic Ach receptors

24

What are the clinical differences between muscarine and pilocarpine?

Muscarine - Hallucinogen found in magic mushrooms
Pilocarpine - Used to treat dry mouth

25

Which drug is more likely to be used to treat dry mouth?
Muscarine or Pilocarpine?

Pilocarpine

26

What is the pharmacological name for Botulinium A toxin?

Botox

27

What is Botox' mechanism of action?

Attaches to neurones and sends a chemical into the neurone’s cytoplasm, preventing Ach from being released

28

What class of drug is Botulinium A toxin?

Acetylcholine release inhibitor

29

Does Botox act on the pre synaptic or post synaptic membrane?

Presynaptic

30

How is Botox clinically used?

Cosmetic surgery
Treatment of spasms
Treatment of dystonia

31

What class of drug is Pralidoxime?

Cholinsterase reactivator

32

How does Pralidoxime work clinically?

As an antidote to organophosphates in pesticides.

33

What is Pralidoxime's mechanism of action against pesticides?

Pesticides initially inactivate Ach enzyme, meaning Ach increases. Pralidoxime cleaves the bond formed between organophosphate and Ach receptors thus inactivating their effects.

34

What class of drug is Sarin?

Irreversible cholinesterase Inhibitor

35

How does Sarin act on cholinergic receptors?

inhibits cholinesterase causing acetylecholine to build up so that nerve impulses are continually transmitted.

36

What effect does the drug Sarin have on muscle movement?

Causes inability for muscles to relax.

37

What group of chemical products would Sarin be found in?

Organophosphates

38

What would Sarin be used for?

A chemical weapon.

39

What class of drug is Hemicholinium?

Choline reuptake inhibitor

40

What class of drug is Donepezil?

Reversible cholinesterase enzyme inhibitor

41

What is hemicholinium's mechanism of action?

Blocks reuptake of choline via high affinity choline transporter at presynaptic membrane, decreasing amount of Ach that can be made

42

What are the clinical applications of hemicholium?

Not used as a medication but used in research

43

What is donepezil's mechanism of action?

Increases Ach concentration by temporarily stopping it from being hydrolysed.

44

True or false? Donepezil is clinically used for Alzheimers?

True

45

What class of drug does morphine belong to?

Analgesic

46

What class of drug is Bethamethasone?

Glucocorticoid nuclear receptor agonist/ Anti-inflammatory

47

What is bethmethasone's mechanism of action?

Mimics action of cortisol by altering gene expression which decreases the supply of arachidonic acid-> reducing inflammation

48

What is the phamacological name for Paracetamol?

Acetaminophen

49

What is the trivial/ brand name for Acetaminophen?

Paracetamol

50

What is paracetamol's mechanism of action?

Blocks production of prostaglandins by inhibiting COX

51

What drug classes does Paracetamol belong to?

COX inhibitor/Analgesic/Anti-inflammatory

52

What class of drug is Prednisolone?

Glucocorticoid
Anti-inflammatory

53

What is Prednisolone clinically known for?

It is the most commonly prescribed corticosteroid

54

What is Prednisolone's mechanism of action?

Binds to cytosolic receptors to inhibit leukocyte infiltration, stops inflammatory mediators.
Thought to also act via lipocortins, phospholipase A2 inhibitory proteins which control prostaglandin and leukotrienes production.

55

What class of drug is Chlorphenamine?

H1 antagonist

56

What is the clinical purpose of Chlorphenamine?

Used in the treatment of rhinitis, urticaria, allergy, common cold, asthma and hay fever.

57

What is Chlorphenamine's mechanism of action?

Competes with histamine for normal H1 receptor sites on effector cells, which subsequently leads to temporary relief of negative symptoms brought on by histamine.

58

What class of drug is Diclofenac?

NSAID/ Anti-inflammatory /Analgesic/ Antipyretic

59

What is morphine's mechanism of action?

Mimics endogenous opoids on mu opoid receptors

60

What are opoids?

The body's natural pain killer

61

What is Diclofenac's mechanism of action?

Inhibits COX thus inhibiting prostaglandin synthesis. May also inhibit bacterial DNA synthesis.

62

What is a common side effect of Diclofenac?

GI Complaints.

63

What class of drug is hydrocortisone?

Glucocorticoid/ Anti-inflammatory

64

What are the clinical applications of hydrocortisone?

Used to treat people who lack naturally generated cortisol.

65

What are hydrocortisone's mechanisms of action?

Binds to the cytosolic glucocorticoid receptor-> the newly formed receptor-ligand complex translocates itself into the cell nucleus-> binds to many glucocorticoid response elements (GRE) in the promoter region of target genes, inhibiting prostaglandins and leukotrienes.

66

What class of drug is codeine?

Opiate Receptor Agonist/ Analgesic/ Anti-diarrhoea

67

How is codeine clinically used?

Pain killer, cough medicine, anti-diarrhoea

68

How is codeine metabolised in the stomach?

It is converted into morphine in the stomach

69

What classes of drug does Pethidine belong to?

Opiate Receptor Agonist/ Analgesic

70

What are the major side effects of Pethidine?

Respiratory depression and Bradycardia

71

What are Pethidine's mechanisms of action?

Mimics the actions of endogenous neuropeptides primarily via kappa opioid receptors (but also via mu- receptors), producing the characteristic morphine -like effects.

72

What classes of drug does Tramadol belong to?

Opioid receptor agonist/ Multi-target analgesic

73

What is Tramadol's mechanism of action?

Acts on mu-opioid GPCRs and decreases intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters is inhibited.

74

How is tramadol used in clinical practise?

A very strong painkiller

75

What class of drug does Arnica Motana belong to?

Analgesic/ anti-inflammatory

76

Where is Arnica Motana commonly used?

Homeopathic remedies

77

What is Arnica Motana's mechanism of action?

Affects transcription factor human telomerase.

78

What class of drug is aspirin?

COX-1 inhibitor/ NSAID/Anti-pyretic/Analgesic.

79

How is aspirin used clinically?

Blood Thinner, Painkiller

80

What is aspirin's mechanism of action?

Irreversibly inhibits COX-1 and modifies the enzymatic activity of COX-2 which is required for prostaglandin and thromboxane synthesis.

81

What is the normal role of prostaglandins?

To promote inflammation

82

What is the normal role of thromboxane?

Aggregates platelets for clotting.

83

What class of drug is Ibuprofen?

COX-2 inhibitor/ NSAID/Anti-pyretic/Analgesic

84

What is ibuprofen's mechanism of action?

Inhibits COX-2 enzyme, so inhibits production of prostaglandins

85

What is the strength of ibuprofen in relation to other NSAIDs?

It is weaker

86

What class of drug is naproxen?

COX-1 and COX-2 inhibitor/ NSAID/Anti-pyretic/Analgesic

87

What is naproxen's mechanism of action?

Inhibits enzymes so less prostaglandins for inflammation. Mechanism is poorly understood.

88

What class of drug is Rifampicin?

Antibiotic

89

What is the alternative name for Rifampicin?

Rifadin

90

How is Rifampicin clinically used?

Used to Treat Bacterial Infections

91

What is Rifampicin's mechanism of action?

Inhibits RNA polymerase and blocks the formation of bonds in the RNA backbone

92

What class of drug is Ketaconazole?

Fungal lanosine demethylase inhibitor

93

What class of drug is Nizoral?

Fungal lanosine demethylase inhibitor

94

What is the alternative name for Nizoral?

Ketaconazole

95

What is the alternative name for Ketaconazole?

Nizoral

96

How is ketaconazole clinically used?

Treats Fungal Infections

97

What is ketaconazole's mechanism of action?

Inhibits the synthesis of ergosterol, creating pores in the fungal cell membrane

98

What class of drug is Amoxicillin?

Antibiotic

99

How is Amoxicillin clinically used?

Often used in middle ear infections, pneumonia, skin infections, UTIs etc.

100

What is Amoxicillin's mechanism of action?

Binds to the penicillin binding proteins 1A located inside of the bacterial wall, inhibiting cell wall synthesis leading to cell lysis

101

What class of drug is Clarithromycin?

Antibiotic

102

How is Clarithromycin used clinically?

Used in pneumonia, H pylori infections, Lyme Disease

103

What is Clarithromycin's mechanism of action?

Binds to rRNA, inhibiting the translation of peptides in bacteria.

104

What classes of drug does Metronidazole belong to?

Antibiotic/Antiprotozoal

105

How is Metronidazole used clinically?

Used for PID, C diff, Bacterial vaginosis

106

What is Metronidazole's mechanism of action

Inhibits nucleic acid synthesis by disrupting the DNA of microbial cells

107

What type of antibiotic is Amoxicillin?

Bacteriocidal

108

What type of antibiotic is Metronidazole?

Bacteriostatic

109

What class of drug is Tamoxifen?

Oestrogen nuclear hormone receptor antagonist

110

What is Tamoxifen's mechanism of action?

Pro Drug which competitively antagonises oestrogen receptors

111

What is Tamoxifen clinically used for?

To reduce the size of oestrogen dependant breast tumours

112

What is are the pharmaceutical names for Yasmin?

Ethinylestradiol/Levenorgestrel

113

How is Levenorgestrel clinically used?

Oral contraceptive

114

What is Ethinylestradiol's mechanism of action?

Increases formation of sex hormone binding globulins, thyroid binding globulins and suppresses follicle stimulating hormone?

115

What is Levenorgestrel's mechanism of action?

Increases formation of sex hormone binding globulins, thyroid binding globulins and suppresses follicle stimulating hormone?

116

How is Ethinylestradiol clinically used?

Oral contraceptive

117

What pharmacological effect does ethanol have on health?

Cellular depressant used as behaviour altering substance

118

What is ethanol's believed mechanism of action?

Believed to act on to alter both GABA and glutamate receptors

119

What is the alternative name for diamorphine?

Heroin

120

What class of drug is heroin?

Mu Opiate Receptor Agonist/ Analgesic

121

True or false? Diamorphine is a recreational drug.

True (a.k.a. Heroin)

122

What is diamorphine's mechanism of action?

Agonist to beta-endorpine, dynorphin, leu-enkephalin and met-enkephalin, so reduces pain

123

What class of drug is cocaine?

Noradrenaline reuptake inhibitor/sodium channel blocker

124

Is codeine a recreational drug?

Yes

125

What is codeine's mechanism of action?

Inhibits the re-uptake of seratonin, dopamine and noradrenaline, so greater concentrations are available causing euphoric effects.

126

What is interesting about codeine?

Can cross the blood brain barrier

127

What type of drug is nicotine?

Nicotinic cholinergic receptor agonist

128

What is nicotine's mechanism of action?

Binds to nicotinic acetylcholine receptors on dpoaminergic neurons in the cortico-limbic pathways of the brain. This leads to release of dopamine into synpase - produces euphoric and addictive properties of nicotine.

129

How does nicotine have an effect on adrenaline levels?

It binds to nicotinic receptors in adrenal medulla, depolarising them, which causes release of adrenaline.

130

What type of drug is atenolol?

Beta adrenoreceptor antagonist
(Beta Blocker)

131

What effect does atenolol have on the heart?

Reduces heart rate, blood pressure and cardiac output

132

What is atenolol's mechanism of action?

Competes with adrenalin and noradrenalin for binding at beta-1 adrenergic receptor thus reduced heart rate

133

What function do propanolol and atenolol have in common?

They're both beta blockers (beta adrenoreceptor antagonists)

134

How is propanolol used clinically?

Treatment of ischemic heart disease, heart failure.

135

What is propanolol's mechanism of action?

Non-selective beta blocker, blocks action of both adrenalin and noradrenalin thus reducing heart rate.

136

What type of drug is bendro-flumethiazide?

Sodium chloride co-transporter inhibitor/ Thiazide diuretic

137

How is bendro-fumethiazide used clinically?

Used to treat high blood pressure

138

What is bendro-flumethiazide's mechanism of action?

Inhibits sodium re-absorption

139

What class of drug is amiodarone?

Potassium Channel Blocker
(Vaughan-Williams Class III antiarrythmic agent)

140

How is amiodarone clinically used?

To treat ventricular and atrial fibrillation

141

What is amiodarone's mechanism of action?

Blocking K+ channels delays cell repolarisation, so increase in length of action potential and increase in effective refractory period so decreased heart rate.

142

Does amiodarone only have an effect on K+ receptors?

No.

Capable of blocking sodium, potassium, calcium and beta receptors.

143

What type of drug is Captopril?

ACE inhibitor

144

What does the 'ACE' in 'ACE inhibitor' stand for?

Angiotensin converting enzyme

145

How is captopril used clinically?

Treatment of high blood pressure

146

What is captopril's mechanism of action?

Prevents Angiotensin I being converted to Angiotensin II by inhibiting angiotensin converting enzyme.

This decreases the water retentive and vasodilative effects of angiotensin II so decreases blood pressure.

147

What type of drug is verapamil?

Calcium Channel Blocker

148

How is Verapamil used clinically?

Treatment of high blood pressure and angina

149

What is Verapamil's mechanism of action?

Antagonises calcium channels, so blocks the influx of calcium across the cell membrane of arterial smooth muscle and myocardial cells.
Reduced afterload so reduced blood pressure

150

What type of drug is digoxin?

Sodium potassium ATPase inhibitor

151

How is digoxin used clinically?

Treats low blood pressure

152

What is digoxin's mechanism of action?

Causes a reversal of the ATPase pump so increased amounts of calcium during each action potential in cardiac muscle. Increased contractility without increasing heart energy expenditure

153

What type of drug is Phenoxybenzamine?

Alpha adrenoceptor antagonist/ Antihypertensive

154

What is Phenoxybenzamine clinically used for?

Increasing blood pressure

Controlling manifestations of autonomic hyperreflexia in patients with spinal cord transection

155

What is Phenoxybenzamine's mechanism of action

Blocks alpha receptors, leading to a muscle relaxation and a widening of the blood vessels. This widening results in a lowering of blood pressure.

156

What type of drug is Prazosin?

Alpha adrenoceptor antagonist

157

How is Prazosin used clinically?

Treats hypertension and congestive heart failure

158

What is Prazosin's mechanism of action?

Inhibits postsynaptic a-1 adrenoceptors on vascular smooth muscle, inhibiting the vasoconstriction that circulating adrenaline and noradrenaline would cause, resulting in peripheral vasodilation.

159

What type of drug is atropine?

Muscarinic cholinergic receptor anatagonist

160

What is atropine clinically used for?

Panic disorders (reduces sweating and spasms)

Increases heart rate

161

What is atropine's mechanism of action?

Binds to Ach receptors, preventing the binding and action of Ach.
Reduces action of the parasympathetic nervous system which results in dilated pupils and increased heart rate.

162

What type of drug is norepinephrine?

Alpha adrenoreceptor Agonist

163

What is norepinephrine more commonly known as?

Adrenaline

164

When is norepinephrine used clinically?

In emergency situations
For life-threateningly low blood pressure

165

What is norepinephrine's mechanism of action?

Acts on alpha-1 adreno receptors in blood vessels to cause vasoconstriction and increase blood pressure

166

What class of drug is epinephrine?

Non-selective adrenergic agonist

167

When is Epinephrine clinically administered?

In cases of Anaphylaxis, Cardiac Arrest and Superficial bleeding

168

What is Epinephrine's mechanism of action?

Acts on all major subtypes of adrenergic receptors causing a multitude of effects including increased heart rate.

169

What type of drug is dobutamine?

Beta-adrenoreceptor agonist

170

What is Dobutamine's mechanism of action?

Directly stimulates beta-1 receptors of the heart to increase myocardial l contractility and stroke volume - leading to increased cardiac output

171

What are the side effects of Dobutamine?

Produces mild chronotropic, hypertensive, arrhythmogenic and vasodilative effects.

172

What type of drug is Isoprenaline?

Non-selective beta 1 and 2 adrenergic agonist

173

How is isprenaline used clinically?

Treatment of bradycardia (slow heart rate), heart block, and rarely for asthma

174

What is the trivial/brand name for salbutamol?

Ventolin Inhaler

175

What is the chemical name for ventolin?

Salbutamol

176

What type of drug is salbutamol?

Short Acting Beta-2 adrenoreceptor agonist (SABA)

177

What is salbutamol clinically used for?

Treats asthma

178

What is salbutamol's mechanism of action?

Stimulation of SABA receptors leads to high levels of cyclic AMP which relaxes bronchial smooth muscle and decreases airway resistance. Also decreases release of histamine.

179

What type of drug is salmeterol?

Long Acting Beta adrenoceptor agonist (LABA)

180

What is salmeterol used for clinically?

Treats asthma and COPD symptoms

181

What is the difference between salbutamol and salmeterol?

Salbutamol is a short acting B2 adrenoreceptor agonist

Salmeterol is a long acting B2 adrenoreceptor agonist

182

What type of drug is orlistat?

Lipase inhibitor

183

What is orlistat used for clinically?

Treating obesity

184

What is orlistat's mechanism of action?

Prevents breakdown of triglycerides in the intestine, so they are simply excreted.

185

What type of drug is atorvostatin?

Statin/ Competitive inhibitor of HMG-CoA reductase

186

What is atorvostatin's mechanism of action?

Inhibits HMG-CoA which normally aids in cholesterol synthesis. Decreased LDL uptake by hepatocytes. Also reduced blood levels of triglycerides and increases levels of HDL. (Cholesterol excreted)

187

How is atorvostatin used clinically?

Lowers blood cholesterol and treats CVD

188

What type of drug is Bezafibrate?

Fibrate

189

What is Bezafibrate used for clinically?

To lower blood cholesterol and triglycerides

190

What is Bezafibrate's mechanism of action?

Stimulates the action of 2 enzymes ( lipoprotein lipase and hepatic lipase) that break down triglycerides. Reduces production of triglycerides in the liver.

191

What type of drug is Hydroxycobalamin?

Co-enzyme/ Vitamin precursor

192

What is Hydroxycobalamin used for clinically?

Used to treat Vitamin B12 deficiency (megaloblastic anaemia)

193

What is vitamin B9 more commonly known as?

Folic acid/ Folate

194

What is vitamin B9 used for clinically?

Used to treat Folic Acid deficiency (megaloblastic anaemia), given in pregnancy

195

What is vitamin B9's mechanism of action?

Biochemically inactive so it’s converted to tetrahydrofolic acid and methyltetrahydrofolate by dihydrofolate reductase which are used to maintain normal erythropoiesis.

196

What type of drug is Ferrous sulphate?

Oxidation Modulator

197

What is Ferrous sulphate used for clinically?

Used to treat iron-deficiency anaemia

198

What is Ferrous sulphate's mechanism of action?

Passes through the GI mucosal cells directly into the blood and binds to transferrin. This transports iron into the bone marrow where it is incorporated into haemoglobin.

199

How is Ferrous sulphate best absorbed?

With vitamin C

200

What type of drug is warfarin?

Vitamin K Antagonist/ Anti-coagulant

201

How is warfarin used clinically?

Used to treat blood clots

202

What is warfarin's mechanism of action?

Depletes the recycling of Vitamin K epioxide back into active Vitamin K by inhibiting an enzyme which aids in the reaction. Therefore inhibits the vitamin K dependent synthesis of clotting factors.

203

What type of drug is clopidogrel?

Anti-platelet drug/ Pro-drug

204

What is clopidogrel used for clinically?

Used to protect against strokes and heart attacks

205

What is clopidogrel's mechanism of action

Irreversibly inhibits a receptor called P2Y, an ADP chemoreceptor on platelet cell membranes.

Platelet activation and cross-linking by fibrin can no longer happen so platelets can't stick together and clots can't form.

206

What type of drug is Heparin?

Anti-coagulant

207

What is heparin used for clinically?

Treating DVT, pulmonary embolisms and venous thromboembolisms

208

What are the two types of heparin?

Unfractionated (UFH)
Low molecular weight (LMWH)

209

How does unfractionated heparin work?

UFH binds to anti-thrombin causing conformational change which increases affinity for clotting factor FXa and thrombin and inactivates them. Forms a tertiary complex between AT, thrombin and heparin to inactivate thrombin.

210

How does low molecular weight heparin work?

It forms the same complex as UFH, but can only inactivate FXa (not thrombin)

211

What type of drug is Lepirudin?

Anti-coagulant

212

How is Lepirudin used clinically?

DISCONTINUED - Was used in patients previously treated with heparin, but have developed heparin-induced thrombocytopenia.

213

What is Lepirudin's mechanism of action?

Binds to thrombin, directly inhibiting blood clotting.

214

What type of drug is Chlorpromazine?

Dopamine Antagonist/ Anti-emetic/ Anti-Psychotic

215

What is chlorpromazine's mechanism of action?

Blocks the action of dopamine in the chemical trigger zone, the cortical and limbic areas of the brain as well as the gut.

216

Does chlorpromazine only target dopamine receptors?

Nope.
Also blocks action of 5-HT, histamine etc...

217

What is chlorpromazine's mechanism of action?

Increasing gut motility
Relieving nausea
To treat psychosis

218

What type of drug is Domperidone?

D2 and D3 Antagonist/ Anti-emetic

219

What is Domperidone clinically used for?

Increases GI peristalsis and lactation

220

What is Domperidone's mechanism of action?

Blocks dopamine receptors at the chemoreceptor trigger zone and in the duodenum.

221

What type of drug is Metoclopramide?

Dopamine D2 Receptor Antagonist/ Antiemetic

222

What is Metoclopramide's mechanisms of action?

Blocks the action of dopamine in the chemical trigger zone

223

What is metoclopramide used for clinically?

Relieving nausea and increasing gut motility

224

What type of drug is Perphenazine?

D2 receptor Antagonist/ Anti-emetic/ Anti-Psychotic/ Phenothiazine.

225

What is Perphenazine used for clinically?

Treats violent morning sickness in pregnant women and the positive symptoms of Schizophrenia

226

What is Perphenazine's mechanism of action?

Acts at all levels of the CNS, though the specific sites and actions are unknown.

227

What type of drug is Cinnarizine?

Selective histamine antagonist/ Calcium channel blocker/ Anti-emetic

228

What is Cinnarizine's mechansim of action?

Binds to receptors (dopamine, histamine) to inhibit smooth muscle contraction

229

What type of drug is Cyclizine?

H1 receptor antagonist/ Anti-emetic

230

What is Cyclizine's mechanism of action?

Mechanism of action to reduce nausea is poorly understood, may act at the CTZ.

231

What type of drug is promethazine?

Competitive H2 receptor antagonist/ Anticholinergic/ Sedative/ Anti-emetic

232

Why type of drug is Hyoscine?

Muscarinic antagonist

233

What is Hyoscine used for clinically?

Used for treating spasms in the G.I. and G.U. tracts and treating motion sickness

234

What is Hyoscine's mechanism of action?

Inhibits communication between the vestibule and vomiting centre

235

What type of drug is Ondansetron

Serotonin 5-HT3 receptor antagonist/ anti- emetic

236

What is Ondansetron used for clinically?

Used particularly in chemotherapy, postoperation and radiation

237

What is Ondansetron's mechanism of action?

Prevents the action of sertonin on the vagus nerve and in the CTZ.

238

What type of drug is Esomeprazole?

Proton-pump inhibitor (PPI)

239

What is Esomeprazole used for clinically?

Peptic ulcers and reflux

240

What is Esomeprazole's mechanism of action?

Inhibits an enzyme involved at the H+/K+ ATPase pump at the secretory surface of the gastric parietal cell resulting in reduced secretion of gastric acid.

241

What is special about Esomeprazole and Omeprazole?

They're mirror images/ chiral isomers

242

What type of drug is Omeprazole?

PPI

243

What is omeprazole clinically used for?

Peptic ulcers and reflux

244

What is omeprazole's mechanism of action?

Reduced secretion of gastric acid through H+/K+ ATPase by inhibiting an enzyme involved at the pump at the secretory surface of the gastric parietal cell.

245

What type of drug is Ranitidine?

H2 receptor antagonists

246

What is Ranitidine used for clinically?

Peptic ulcers and reflux

247

What is Ranitidine's mechanism of action?

Stops histamine stimulation of parietal cells.

248

What type of drug is Magnesium Trisilicate?

Antacid/ Laxative

249

What is Magnesium Trisilicate's mechanism of action?

Neutralises pH of gastric juice as it is an alkali. Also coats the GI mucosa protecting it in the future.

250

What type of drug is Misoprostol?

Prostaglandin

251

How is Misoprostol used clinically?

Prescribed with NSAIDs to protect stomach from injury.
Used in inducing labour and can also cause abortions.

252

What is Misoprostol's mechanism of action?

Replaces the PGs lost in NSAID use. Stimulates increased secretion of the protective mucus that lines the GI tract and increases mucosal blood flow, increasing mucosal resistance to injury. Also inhibits gastric acid and pepsin secretion.

253

What type of drug is Gaviscon?

Antacid

254

What is Gaviscon clinically used for?

Indigestion

255

What is Gaviscon's mechanism of action

Contains alkaline ions which neutralise stomach gastric acid. Contains an alkaline ion (bicarbonate but may also be hydroxide) and a counterion (calcium/ sodium)

256

What type of drug is Azathioprine?

Immunosuppressive/ / Pro-drug

257

What is Azathioprine used for clinically?

Used in organ transplantation and autoimmune diseases

258

What is Azathioprine's mechanism of action?

Converted into mercaptopurine which inhibits an enzyme required for the synthesis of DNA.. Most strongly affects proliferating cells, such as the T and B cells.

259

What type of drug is Cyclosporine?

Immunosuppressant

260

What is Cyclosporine used for clinically?

Used to prevent organ transplantation rejection (often administered IV)

261

What is Cyclosporine's mechanism of action?

Exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-G1 phase of the cell cycle. T-lymphocytes are preferentially inhibited. T1-helper cell is the main target. Inhibits interleukin release.

262

What type of drug is Levodopa?

Dopamine precursor

263

What is Levodopa used for clinically?

Used in treatments of Parkinson's, causes lots of side effects.
Side effects include schizophrenic symptoms

264

What is levodopa a precursor for?

The neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine.

265

What type of drug is Imipramine?

Catecholamine uptake inhibitor/ Anti-depressant

266

What is Imipramine's mechanism of action?

Binds the sodium-dependent serotonin and norepinephrine transporters, reducing the re-uptake of norepinephrine and serotonin by neurones.

267

What is Imipramine used for clinically?

Depression

268

What type of drug is Dopamine?

Dopamine receptor agonist/ Catecholamine

269

What is Dopamine's mechanism of action?

Acts in the brain for reward motivated behaviour. Also acts in various other places around the body.

270

What type of drug is Fluoxetine?

Selective Serotonin reuptake inhibitor (SSRI)/ Antidepressant

271

What is the trivial/ brand name for fluoxetine?

Prozac

272

What is Prozac's mechanism of action?

Metabolized to norfluoxetine, it blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors.

273

What is better about fluoextine in comparison to other SSRIs?

It has fewer extra-pyramidal side effects

274

What type of drug is Phenelzine?

Monoamine oxidase inhibitor/ Antidepressant/ Anxiolytic

275

What is Phenelzine's mechanism of action?

Inhibits the enzyme which breaks down various neurotransmitters. Leads to an increase in the amount of neurochemicals causing anti-depressive and anxiolytic effects

276

What type of drug is Diazepam?

GABA Receptor Agonist/ Benzodiazepine/ Muscle relaxant

277

What is an alternative name for Diazepam?

Valium

278

What is Diazepam used for clinically?

Used to treat anxiety.

279

What is Valium's mechanism of action?

Attaches to GABA on the receptors, increasing the total conduction of chloride ions across the membrane, making firing less likely.

280

What type of drug is Buspirone?

5HT partial receptor agonist

281

What is an alternative name for Buspirone?

Azapirone Psychotropic Drug

282

What is Buspirone used for clinically?

Treats generalised anxiety disorder

283

What is Buspirone's mechanism of action?

Increases the action of serotonin which causes anxiolytic effects. Also antagonises dopamine and nordrenalin receptors. Less risk of dependence than benzodiazepines's or barbituates.

284

What type of drug is Chlopromazine?

Dopamine Receptor Antagonist/ Antipsychotic

285

What is Chlopromazine used for clinically?

Treats Schizophrenia and Bipolar disorder

286

What is Chlopromazine's mechanism of action?

Blocks D1-D4 and 5-HT1 and 5-HT2 receptors (and others), causing anxiolytic and anti-aggressive properties.

287

Why is Chlopromazine a 'typical antipsychotic'?

Less extrapyramidal side effects than other antipsychotics

288

What type of drug is Haloperidol?

Dopamine Receptor Antagonist/ Antipsychotic

289

What is C used for clinically?

Treats schizophrenia and Tourette's

290

What is Haloperidol's mechanism of action?

Binds to D2 and alpha1 receptors to antagonise them thus reducing the availability of dopamine.

291

Why is Haloperidol a 'typical psychotic'?

Little affinity for histamine and Ach receptors causes less extrapyramidal side effects.

292

What type of drug is Risperidone?

Dopamine and 5HT Antagonist/ Multi-target, atypical antipsychotic

293

What is Risperidone used for clinically?

Treats Schizphrenia, Bipolar and also used in people with Autism.

294

What is Risperidone's mechanism of action?

Long half life on Dopamine Receptors. Blocks 5HT for negative symptom control. Also acts on adrenalin receptors and Histamine receptors to cause drowsiness and also aid with symptom control

295

What type of drug is Amitryptyline?

Noradrenaline/5HT reuptake inhibitor/ Tricyclic Antidepressant

296

What is Amitryptyline used for clinically?

Treats generalised anxiety major depressive disorder.

297

What is Amitryptyline's mechanism of action?

Blocks the reuptake of noradrenaline and 5HT to increase the availability of the neurotransmitters. Little effect on dopamine receptors.

298

What type of drug is Lithium?

Sodium Analogue/ Mood Stabiliser

299

What is Lithium used for clinically?

Counteracting both mania and depression

300

What is Lithium's mechanism of action?

Precise mechanism currently unknown. Possibly interacts with transport of monovalent or diavalent cations in neurons. Also changes glutamate currents.

301

What type of drug is Methylphenidate?

Noradrenaline/Dopamine Releaser.
Noradrenalin-Dopamine Reuptake Inhibitor (NDRI)/ CNS Stimulant

302

What is the alternative name for Methylphenidate?

Ritalin

303

What is Ritalin used for clinically?

Treats ADHD and narcolepsy

304

What is Ritalin's mechanism of action?

Increases availability at receptors by blocking re-uptake. Shares part of structure with catecholamines.

305

What type of drug is Dexamefetamine ?

Noradrenaline releaser/ CNS stimulant and amphetamine enantiomer.

306

What is Dexamefetamine clinically used for?

Prescribed for ADHD and narcolepsy

307

What type of drug is Naloxone ?

Opiate Receptor Antagonist

308

What is Naloxone clinically used for?

Reversing the effects of opoid medication.

309

What is Dexamefetamine 's mechanism of action?

Agonising GPCR causes the release of dopamine, norepinephrine and serotonin.

310

What is Naloxone's mechanism of action?

Competitively antagonising opiod receptors

311

What is oxygen used for clinically?

Used as an emergency treatment for severely low oxygen levels

312

What is important about oxygen administration?

Various concentrations available; have to be careful with people who have chronic low oxygen because this can make their levels too high

313

What type of drug is Thalidomide?

Anti-angiogenic/Immunosuppressive/VEGF inhibitor

314

What is Thalidomide used for clinically?

Used for treatments of tumours
2 enantiomers - one that is effective against morning sickness and the other that is teratogenic

315

Are the mechanisms of Thalidomide understood?

No

316

What type of drug is the tetanus booster?

Antibody stimulator

317

What are the tetanus booster's mechanisms of action?

Inactivated toxic compounds from micro-organisms are injected to artifically activate immunization against tetanus

318

What type of drug is Lidocaine?

Sodium channel blocker/ Anaesthetic

319

What is lidocaine used for clinically?

Local anaesthetic agent used in dental procedures, can be combined with adrenaline

320

What is lidocaine's mechanism of action?

Mimics the actions of endogenous neuropeptides primarily via kappa opioid receptors (but also via mu- receptors), producing the characteristic morphine -like effects.

321

What class of drug is methicillin?

Transpeptidase inhibitor

322

What is methiciliin's mechanism of action?

Inhibits bacterial cell wall synthesis by binding to the enzyme used to cross link the peptide used in peptidoglycan synthesis.

323

What is methicillin used for clinically?

It isn't. Its role has been replaced by flucloxacillin and dicloxacillin.

324

What class of drug is cefuroxime?

transpeptidase inhibitor

325

What is cerfuroxime's mechanism of action?

Binds to and inhibits the enzyme that cross links the peptide chain for peptidoglycan.

326

What pathogens is cerfuroxime targeted at?

Beta-lactamase-producing H.influenza and N.gonorrhoea.

327

What conditions is cerfuroxime used for clinically?

Sinusitis
Ear infections
Lower respiratory tract infections
Urinary infections

328

What are common side effects of cerfuroxime?

Hypersensitivity reactions
GIT disturbances

329

What class of drug is benzylpenicillin?

Transpeptidase inhibitor

330

Give examples of transpeptidase inhibitors

Methicillin
Cerfuroxime
Benzylpenicillin

331

Are transpeptidase inhibitors bacteriostatic or bactericidal?

Bactericidal

332

What is the common mechanism of action for transpeptidase inhibitors?

Binding to and inhibiting the enzyme that cross links the peptide chain for peptidoglycan, a component of the cell wall.

333

What is benzylpenicillin used for clinically?

Streptococcal, gonococcal and meningococcal infections
Anthrax
Diphtheria
Gangrene

334

What infectious agent is resistant to benzylpenicillin?

Staphylococcus

335

Is oxytetracycline a broad or narrow spectrum antibiotic?

Broad spectrum

336

What class of drug is oxytetracycline?

30s inhibitor

337

What class of drug is erythromycin?

50s inhibitor

338

What class of drug is gentamicin?

30s/50s inhibitor

339

Are 30s/50s inhibitors bacteriostatic or bactericidal?

Bacteriostatic

340

What is gentamicin's mechanism of action?

Causes misreading of the mRNA message via abnormal codon: anticodon recognition. This then leads to the production of abnormal proteins.

341

What is erythromycin's mechanism of action?

Inhibits the translocation of the transfer RNA from the A site to the P site.

342

If gentamicin is used for staph infections, what must it be used with?

A beta-lactam antibiotic

343

What class of drug is rifampicin?

DNA dependent RNA polymerase inhibitor

344

What is rifamicin's mechanism of action?

Inhibits bacterial but not human DNA dependent RNA polymerase, causing reduced RNA synthesis in the bacterial cell.

345

Is rifampicin bacteriostatic or bactericial?

Bactericidal

346

What is rifampicin used for clinically?

Tuberculosis
Leprosy
Meningococcal meningitis prophylaxis
Endocarditis
Legionnaires
Serious staph infections

347

What are the side effects of rifampicin?

Reduces the effect of anticoagulants and oral contraceptives

348

What class of drug is trimethoprim?

Folate antagonist

349

What is trimethoprim's mechanism of action?

Inhibits dihydrofolate reductase and therefore the conversion of folate to tetrahydrofolate. This stops DNA synthesis.

350

What is trimethoprim used for clinically?

Prostatitis
UTIs
Respiratory infections

351

What class of drug is sulfamethoxazole?

PABA analogue

352

What class of drug is vancomycin?

Peptidoglycan inhibitor

353

What is sulfamethoxazole's mechanism of action?

Completely inhibits dihydropteroate synthetase, stopping DNA synthesis

354

What is vancomycin's mechanism of action?

Inhibits removal of an amino acid from a building block in peptidoglycan formation, so the building blocks don't have enough energy to link up.

355

What is vancomycin used for clinically?

MRSA infections
Pseudo-membranous colitis

356

What class of drug is colistin?

Phospholipid detergent

357

What is colistin's mechanism of action?

Penetrates into and disrupts the bacterial cell membrane. It also messes up the membrane's permeability.

358

What is colistin used for clinically?

Infections caused by sensitive strains of gram negative bacilli.

359

What class of drug is ciprofloxacin?

Topoisomerase II inhibitor

360

Is colistin bacteriostatic or bactericidal?

Bactericidal

361

Is ciprofloxacin bacteriostatic or bactericidal?

Bactericidal

362

What is ciprofloxacin's mechanism of action?

Inhibits topoisomerase II and IV which are needed for DNA replication, transcription, repair, supercoiling repair and recombination in bacteria.

363

What is ciprofloxacin used for clinically?

UTIs
Cystitis
Prostatitis
Lower respiratory tract infections
Sinusitis
Skin bone and joint infections

364

What class of drug is fusidic acid?

Translocation inhibitor

365

What is fusidic acid's mechanism of action?

Interferes with bacterial protein synthesis by preventing translocation of the elongation factor G (EF-G) from the ribosome

366

Is fusidic acid bacteriostatic or bactericidal?

Bacteriostatic

367

What class of drug is ibruprofen?

NSAID

368

What is ibruprofen's mechanism of action?

Reversible inhibition of COX 1, weak inhibition of COX 2

369

What class of drug is acyclovir?

Antiviral

370

What is acyclovir's mechanism of action?

Converted by viral and host cell kinases to acyclovir triphosphate which selectively inhibits viral DNA polymerase.

371

What is acyclovir used for clinically?

Herpes simples and herpes zoster infections

372

What class of drug is amantidine?

Antiviral
Antiparkinsonian

373

What is amantidine's mechanism of action?

Believed to increase dopamine release from nerve endings in the striatum. May also have antimuscarinic effects.

374

What is amantidine used for clinically?

Parkinson's disease
Dyskinesia associated with levodopa therapy

375

What class of drug is diamorphine?

Analgesic

376

What is diamorphine's mechanism of action?

Activates opioid receptors in the brain and spinal cord to inhibit pain transmission and modify central perception of pain.

377

What is diamorphine used for clinically?

Moderate to severe chronic and post-operative pain
Epidural anaesthesia
Neuropathic pain
Painful cough treatment
Diarrhoea

378

What class of drug is amprenavir?

Anti-retroviral, protease inhibitor

379

What is amprenavir's mechanism of action?

Inhibits HIV viral proteinase resulting in non-infectious immature viral particles.

380

What class of drug is phenoxymethylpenicillin?

Antibiotic

381

Is phenoxymethylpenicillin bacteriostatic or bactericidal?

Bactericidal

382

What is phenoxymethylpenicillin's mechanism of action?

Binds to and inhibits the enzyme that cross links the peptide chain of the newly formed 'building block' to the peptidoglycan backbone.

383

What is phenoxymethylpenicillin used for clinically?

Streptococcal, gonococcal, meningococcal infections
Anthrax
Diphtheria
Gas gangrene

384

What can't phenoxymethylpenicillin be used for?

Staph infections

385

What class of drug is Zidovudine?

Anti-retroviral

386

What is zidovudine's mechanism of action?

Phosphorylated into triphosphate form which interferes with viral DNA synthesis

387

What is zidovudine used for clinically?

HIV

388

What is the main problem with zidovudine use?

Resistance is likely to occur
Has to be used with other anti-retrovirals

389

Give examples of antibody production stimulators

MMR vaccine
Influenza vaccine

390

What class of drug is clotrimazole?

Antifungal

391

What is clotrimazole's mechanism of action?

Alters the permeability of the fungal cell wall by binding to phospholipids in the cell membrane. Inhibits sterols needed for cell membrane production.

392

What class of drug is fluconazole?

Antifungal

393

What is fluconazole's mechanism of action?

Inhibits a P450 dependent enzyme which is important in sterol conversion and therefore cell membrane production

394

Is fluconazole fungastatic or fungicidal?

Fungastatic

395

What is fluconazole used for clinically?

Candidiasis
Tinea infections
Crytococcal meningitis
Histoplasmosis
Blastomycosis
Coccidiomycosis

396

What class of drug is Nystatin?

Antifungal

397

What is Nystatin's mechanism of action?

Binds to ergosterol in fungal cell membrane, increasing membrane permeability

398

What is nyastatin used for clinically?

GIT candidiasis

399

What class of drug is amphotericin?

Antifungal

400

What is amphotericin's mechanism of action?

Kills fungi by binding to the ergosterol in the fungal cell membrane, increasing cell membrane permeability

401

What is amphotericin used for clinically?

Candidiasis
meningitis
Histoplasmosis

402

What class of drug is pyrimethamine?

Antimalarial

403

What is pyrimethamine's mechanism of action?

Inhibits the malaria parasite's dihydrofolate reductase (DHFR), interfering with thymidylate synthesis.

404

What is pyrimethamine used for clinically?

Combined with sulfadoxine for treatment of Falciparum malaria.

405

What class of drug is quinine?

Antimalarial

406

What is quinine's mechanism of action?

Thought to inhibit haem polymerase which would normally degrade haem which in itself is toxic to the parasite.

407

What is quinine used for clinically?

Acute attacks of malignant malaria (P. falciparum)

408

What class of drug is artemether?

Antimalarial

409

What is artemether's mechanism of action?

Inhibits falciparum sarcoplasmic endoplasmic reticulum calcium ATPase

410

What is artemether used for clinically?

Uncomplicated falciparum malaria

411

What class of drug is griseofulvin?

Antifungal

412

What is griseofulvin's mechanism of action?

Interacts with polymerised microtubules inhibiting spindle formation

413

What is griseofulvin used for clinically?

Fungal infections of the skin, hair and scalp
Trichophyton infections in children

414

What class of drug is clobetasone?

Anti-inflammatory
Corticosteroid

415

What is clobetasone used for clinically?

Eczema
Dermatitis

416

What class of drug is dacarbazine?

Alkylating anticancer agent

417

What is dacarbazine's mechanism of action?

Appears to exert cytotoxic effects, though other theories include DNA synthesis inhibition.

418

Is dacarbazine cell cycle-phase specific?

No

419

What id dacarbazine used for clinically?

Metastatic malignant melanoma
Secondary line therapy for Hodgkin's disease

420

What class of drug is cyclophosphamide?

Alkylating anticancer agent

421

What is cyclophosphamide's mechanism of action?

Cross-links DNA by forming covalent bonds with guanine residues on each strand which interferes with cell division, thus triggering apoptosis.

422

What is cyclophosphamide used for clinically?

Chronic lymphocytic leukaemia
Soft tissue sarcoma
Osteogenic sarcoma
Ovarian and breast cancers

423

What class of drug is rituximab?

Cytotoxic anticancer agent

424

What is rituximab 's mechanism of action?

Binds to the CD20 antigen which leads to selective killing of B cells

425

What is rituximab used for clinically?

Treatment of CD20 positive non-Hodgkins lymphoma
Chronic lymphocytic leukaemia
Rheumatoid arthritis

426

What class of drug is doxorubicin?

Cytotoxic anticancer agent

427

What is doxorubicin's mechanism of action?

Inhibits DNA and RNA synthesis through topoisomerase II

428

What is doxorubicin used for clinically?

Bladder cancers
Acute leukaemias
Hodgkin and non-Hodgkin lymphoma
Breast, ovarian, bladder and bronchi tumours

429

What class of drug is paclitaxal?

Mitotic inhibitor
Anticancer agent

430

What is paclitaxal's mechanism of action?

Interferes with the normal function of microtubule growth.
Destroys the cell's ability to use its cytoskeleton in a flexible manner.

431

What is paclitaxal used for clinically?

Kaposi's sarcoma
Lung, ovarian and breast cancers

432

What is tamoxifen used for clinically?

Breast cancer chemotherapy

433

What class of drug is tamoxifen?

Oestrogen receptor agonist

434

What is tamoxifen's mechanism of action?

Competes with endogenous oestrogen for the receptor, preventing cell activation and proliferation.

435

What class of drug is 5-fluorouracil?

Antimetabolite
Anticancer drug

436

What is 5-fluorouracil's mechanism of action?

Interferes with the synthesis of dTMP and therefore DNA synthesis.
Gives rise to a fraudulent nucleotide.
Inhibits thymidylate synthetase.

437

What is 5-fluorouracil used for clinically?

Chemotherapy for GI tract, pancreatic and breast cancers
Malignant skin conditions

438

What is important to note about 5-florouracil administration?

High dose regimens should be followed by 'rescue' with folinic acid to minimise effects on bone marrow and Gi mucosa.

439

What is folinic acid?

A form of tetrahydrofolate

440

What class of drug is etoposide?

Anticancer agent

441

What is etoposide's mechanism of action?

Inhibits DNA topoisomerase II, ultimately inhibiting DNA synthesis

442

Is etoposide cell cycle specific?

Yes. It mainly affects S and G2.

443

What is etoposide used for clinically?

Chemotherapy for:
Refractory testicular tumours
Small cell lung cancer
Lymphoma
Non-lymphocytic leukaemia
Glioblastoma multiforme

444

Which drug is the first line treatment of small cell lung cancer?

Etoposide

445

What class of drug is vinblastine?

Vinca alkaloid

446

What is vinblastine's mechanism of action?

Inhibits mitosis at metaphase by binding to tubular in the mitotic spindle, ultimately leading to cell death.

447

What is vinblastine used for clinically?

Chemotherapy for:
Breast cancer
Testicular cancer
Lymphomas
Neuroblastoma
Hodgkin's lymphoma
Non Hodgkin's lymphoma
Mycosis fungicides
Histiocytosis
Kaposi's sarcoma

448

What class of drug is imatinib?

Anticancer
Protein kinase inhibitor

449

What class of drug is tretinoin?

Retinoid

450

What is tretinoin's mechanism of action?

Binds to retinoids acid receptors, promoting detachment of cornified cells and shedding of corneocytes from the follicle

451

What is tretinoin used for clinically?

Acne
Discolouration
Minimising appearance of wrinkles

452

What is imatinib's mechanism of action?

Inhibits protein kinases.

453

What is imatinib used for clinically?

Chemotherapy for:
Chronic myeloid leukaemia
Acute lymphoblastic leukaemia
Myeloproliferative diseases