Pharmacology Flashcards
1
Q
What is the group of drugs used to treat myasthenia gravis?
A
Muscle excitors
2
Q
Name the two drugs used to treat myasthenia gravis
A
Edrophonium/ Tensilon
Pyridostigmine
3
Q
What is the pharmacological name for tensilon?
A
Edrophonium
4
Q
What is the trivial/ brand name for edrophonium?
A
Tensilon
5
Q
What is tensilon?
A
Muscle excitor used to treat myasthenia gravis
6
Q
How does tensilon work?
A
Competitively inhibits acetyl-cholinesterase, preventing breakdown of Ach. In MG will greatly increase muscle function.
7
Q
Why can tensilon act as a test for MG?
A
It’s a temporary drug which will improve muscle function in MG but make other syndromes worse.
8
Q
How does pyridostigmine work against MG?
A
Inhibits the hydrolysis of Ach by competitively inhibiting acetyl-cholinesterase. Results in the increase of Ach.
9
Q
What class of drug is pyridostigmine?
A
Reversible cholinesterase inhibitor
10
Q
What class of drug is tensilon/ endrophonium?
A
Cholinesterase inhibitor
11
Q
Name the main drugs that act as muscle relaxants
A
Tubocurarine
Suxamethonium
Atracurium
12
Q
How does Tubocurarine work?
A
Blocks the receptor site for Ach
Also causes histamine release.
13
Q
How does Suxamethonium work?
A
Depolarises post synaptic membrane so muscle can’t contract.
14
Q
How does Atracurium work?
A
Antagonises neurotransmitter action of Ach by competitively binding with cholinergic receptor sites on the motor end-plate.
15
Q
What is Suxamethonium clinically used for?
A
Induced muscle relaxation/short term paralysis for tracheal intubation
16
Q
What is Atracurium clinically used for?
A
Used adjunctively in tracheal intubation to provide skeletal muscle relaxation.
17
Q
What is Tubocurarine clinically used for?
A
Used as a poison and spider bite antidote.
18
Q
What receptors do Tubocurarine, Suxamethonium and Atracurium all mutually act on?
A
Cholinergic receptors
19
Q
Which of these drugs is a cholinergic agonist?
Tubocurarine
Suxamethonium
Atracurium
A
Suxamethonium
20
Q
What is the are the differences between Suxamethonium and Atracurium as nicotinic cholinergic drugs?
A
Suxamethonium - Depolarising Agonist
Atracurium - Non-depolarising Anatagonist
21
Q
Why is Tropicamide commonly used for lens and retina examinations?
A
Clinically reduces eye movement
22
Q
Name two muscarinic cholinergic receptor agonists
A
Muscarine
Pilocarpine
23
Q
How do muscarinic cholinergic receptor agonists work?
A
Mimics action of the neurotransmitter acetylcholine by binding muscarinic Ach receptors
24
Q
What are the clinical differences between muscarine and pilocarpine?
A
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
