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Phase I Medicine > Pharmacology Part 2 > Flashcards

Pharmacology Part 2 Flashcards

1
Q

List examples of ACE inhibitors

A 
-pril
Enalapril
Lisinopril
Ramipril
Captopril
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2
Q

What is the least common type of ACE inhibitor?

A

Captopril

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3
Q

What are ACE inhibitors’ mechanism of action?

A

Competitively inhibit angiotensin-converting enzyme, stopping angiotensin II production. Angiotensin II usually acts to increase blood pressure.

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4
Q

What class of drug is amiloride?

A

Sodium channel blocker

Antikaliuretic-diuretic agent

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5
Q

What is amiloride’s mechanism of action?

A

Antihypertensive, inhibits sodium reabsorption predominantly in the collecting ducts of the kidneys by binding with the amiloride-sensitive epithelial sodium channels.

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6
Q

What class of drug is furosemide?

A

Loop diuretic

Sodium potassium chloride co-transporter inhibitor

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7
Q

What is amiloride used for clinically?

A

Hypertension

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8
Q

What is furosemide’s mechanism of action?

A

Competitively inhibits the chloride binding site in the thick ascending loop of Henle, preventing sodium transport into the interstitium and therefore keeping water in the tubule to form urine.

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9
Q

What class of drug is bendroflumethazide?

A

Thiazide diuretic

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10
Q

What class of drug is chlortalidone?

A

Monosulfonamyl diuretic

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11
Q

Which drug is used more commonly? chlortalidone or bendroflumethazide?

A

Chlortalidone

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12
Q

Give examples of Sodium chloride cotransporter inhibitors

A

Bendroflumethazide and chlortalidone

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13
Q

What is chlortalidone’s mechanism of action?

A

Inhibits sodium ion transport across in the ascending limb of the loop of Henle, indirectly increasing potassium excretion via the sodium-potassium exchange mechanism

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14
Q

What is bendroflumethazide’s mechanism of action?

A

Inhibits the Na-Cl co-transporter, increasing sodium, chloride, and water excretion.
Inhibits sodium ion transport, increasing potassium excretion.

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15
Q

Give an example of an alpha adrenoreceptor antagonist?

A

Doxazosin

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16
Q

What is doxasozin’s mechanism of action?

A

Selectively inhibits the alpha 1 subtype of alpha adrenergic receptors, blocking vasoconstriction from catecholamines

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17
Q

What is doxazosin used for clinically?

A

Hypertension

Benign prostatic hyperplasia

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18
Q

What class of drug is spironolactone?

A

Potassium sparing diuretic

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19
Q

Give an example of a mineralocorticoid nuclear hormone receptor antagonist

A

Spironolactone

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20
Q

What is spironolactone’s mechanism of action?

A

Inhibits effect of aldosterone by competitively competing for its receptor in the DCT cells.

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21
Q

What are the problems with using spironolactone clincially?

A

It’s a weak diuretic
Slow onset of action
The effect diminishes slowly

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22
Q

Give an example of a carbonic anhydrase inhibitor?

A

Acetazolamide

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23
Q

What is acetazolamide’s mechanism of action?

A

Inhibits carbonic anhydrase leading to a reduction in the availability of hydrogen ions for active transport. This results in an increase in bicarbonate, sodium, potassium and water excretion.

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24
Q

What class of drug is cisplatin?

A

Antineoplastic alkylating agent

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25
What is cisplatin's mechanism of action?
Attaches alkyl groups to DNA bases resulting in DNA fragmentation, inducing nucleotide mis-pairing and stopping synthesis.
26
Give an example of a folate antagonist
Methotrexate
27
What is methotrexate's mechanism of action?
Inhibits folic acid reductase which converts folic acid to tetrahydrofolic acid which is needed for DNA synthesis.
28
How is methotrexate used clinically?
Management of severe, active, classical or definite rheumatoid arthritis
29
What class of drug is phenobarbital?
GABA receptor agonist/ barbiturate
30
What is phenobarbital's mechanism of action?
Acts on GABA receptors to increase synaptic inhibition. This elevates seizure threshold and reduces the spread of seizure activity
31
What is phenobarbital used for clinically?
Management of seizure disorders, excluding absence
32
What class of drug is pethidine?
Opiate receptor agonist
33
What is pethidine's mechanism of action?
Inhibit adenylate cyclase resulting in a decrease in intracellular cAMP, inhibit nociceptive neurotransmitters, and reduce neuronal excitability.
34
What class of drug is mannitol?
Osmotic diuretic
35
What is mannitol's mechanism of action?
Elevates blood plasma osmolarity resulting in enhanced flow of water from tissues into interstitial fluid and plasma. Increases osmolarity of the glomerular filtrate because it is not reabsorbed in the renal tubule.
36
What class of drug is amphetamine?
Non-catecholamine sympathomimetic
37
What is amphetamine's mechanism of action?
Stimulates the release of noradrenaline and dopamine. Agonises central 5-HT receptors Possibly inhibits MAO Can stimulate peripheral noradrenaline release
38
What class of drug is warfarin?
Vitamin K antagonist | Anticoagulant
39
What is warfarin's mechanism of action?
Inhibits vitamin K reductase, reducing levels of the reduced form of vitamin K which is needed for the production of coagulation factors
40
What class of drug is folic acid?
Haematinic agent
41
What is folate's mechanism of action?
Essential for DNA synthesis and cell proliferation, cofactor in synthesis of purines and pyrimidines which are essential in thymidylate synthesis
42
How is folic acid used clinically?
Supplement in pregnancy to avoid spina bifida
43
What is important to note about the administration of folic acid?
It should not be used in undiagnosed megaloblastic anaemias
44
Why should folic acid not be used in vitamin B12 anaemias?
The anaemia may improve but neurological lesions will persist.
45
What is levonorgestrel used for clinically?
Contraceptive
46
What is levonorgestrel's mechanism of action?
Binds to progesterone and oestrogen receptors. Once bound, it slows the frequency of GnRH release from the hypothalamus and blunts the pre-ovulatory LH surge.
47
What is a similar drug to Levonorgestrel?
Desogestrel
48
What type of drug is oxytocin?
Uterine and lactation stimulant
49
What is oxytocin's mechanism of action?
Acts on oxytocin receptors in the smooth muscle of the myometrium. Contracts myoepithelial cells in the post partum mammary gland resulting in 'milk let down'
50
What is oxytocin used for clinically?
Induction or augmentation of labour when uterine muscle isn't functioning properly. Used to prevent/ treat haemorrhage postpartum/ due to incomplete abortion.
51
What type of drug is ethinylestradiol?
FSH inhibitor | Contraceptive
52
What is ethinylestradiol's mechanism of action?
Suppresses the development of the ovarian follicle by inhibiting FSH release from the anterior pituitary.
53
What is ethinylestradiol used for clinically?
Contraception
54
What class of drug is dinoprostone?
Prostaglandin | Uterine stimulant
55
What is dinoprostone's mechanism of action?
Activates PGF2 receptors on uterine smooth muscle
56
What is dinoprostone used for clinically?
Intravaginal gel used to induce pregnant women by softening and dilating the cervix.
57
What must be noted before prescribing flucloxacillin?
Pneumococci, meningococci and gonococci are all resistant.
58
What is flucloxacillin's mechanism of action?
Binds to and inhibits the enzyme that cross-links the peptide chain of the building blocks to the peptidoglycan cell wall.
59
What class of drug is tetracycline?
Antibiotic
60
What is tetracycline's mechanism of action?
Interferes with bacterial cell wall synthesis by competing with tRNA for the A site of the ribosome and reversibly inhibiting its binding to the mRNA codons in the 30s subunit.
61
Is tetracycline bacteriostatic or bactericidal?
Bacteriostatic
62
What is tetracycline used for clinically?
Chlamydia Ricketts Brucella Also effective in infections with mycoplasma and H.influenzae.
63
What class of drug is gentamicin?
Antibiotic | Aminoglycoside
64
What is gentamicin's mechanism of action?
Causes misreading of mRNA message due to abnormal codon:anticodon recognition
65
What is gentamicin used for clinically?
Meningitis | Septicaemia
66
What is a major side effect of gentamicin?
Ototoxicity (can cause deafness in newborns)
67
What type of drug is sodium valproate?
Anticonvulsant
68
What is sodium valproate's mechanism of action?
Dissociates to the valproate ion in the GI tract then binds to and inhibits GABA transaminase. This is thought to result in increased concentrations of GABA
69
What is sodium valproate used for clinically?
Treatment and management of seizure disorders, mania and prophylactic treatment of migraine headache
70
What is ethanol's mechanism of action?
Mimics GABA's effect in the brain by binding to the respective receptors and inhibiting neuronal signalling
71
What is ethanol used for clinically?
To suppress spasms
72
What type of drug is cocaine?
Indirect sympathomimetic
73
What is cocaine's mechanism of action?
Inhibits uptake of noradrenaline, leading to its increased effects (notably vasoconstriction)
74
What is cocaine used for?
Local anaesthetic | Widely used drug of addiction
75
What is a common side effect on cocaine?
Necrosis of nasal septum in addicts who snort it.
76
What type of drug is lithium?
Mood stabiliser
77
What is lithium's believed mechanism of action?
Interferes with membrane ion transport, perhaps including neurotransmitter reuptake
78
What is lithium used for clinically?
Bipolar disorder Mania In combination with other agents in unipolar depression
79
What type of drug is ampicillin?
Antibiotic
80
Is ampicillin bacteriostatic or bactericidal?
Bactericidal
81
What is ampicillin's mechanism of action?
Binds to and inhibits the enzyme that cross links the peptide chain of the building blocks to the peptidoglycan cell wall backbone
82
Is ampicillin a narrow- or broad-spectrum antibiotic?
Broad spectrum
83
What is important to note about ampicillin administration?
Intramuscular Intravenous Slow IV infusion
84
What is the main problem with ampicillin use?
It is inactivated by bacterial beta lactamases
85
Why is clavulanic acid important clinically?
It inhibits beta lactamases so is given with ampicillin
86
What is thalidomide notorious for?
Teratogenic effects
87
What is thalidomide's believed mechanism of action?
May be related to suppression of excessive TNF alpha production
88
What type of drug is thalidomide?
Immunomodulatory agent
89
What is testosterone used for clinically?
Replacement therapy in hypogonadism
90
What are the side effects of testosterone?
Odeoma | Eventual decrease in gonadotropin release -> infertility
91
What is testosterone's mechanism of action?
Converted to dihydrotestosterone which enters cella and interacts with nuclear receptors to initiate transcription of genes.
92
What is somatotropin used for clinically?
Used to treat dwarfism and growth failure
93
What is somatotropin's mechanism of action?
Binds to the human growth hormone receptor GHR which causes recruitment and activation of signalling molecules that contribute to changes in enzyme activity, transport function and gene expression -> growth
94
Is gentamicin bacteriostatic or bactericidal?
Bacteriostatic
95
What type of drug is azathioprine?
Purine metabolism antagonist
96
What is azathiprine's mechanism of action?
Incorporation of thiopurine analogues into the DNA structure -> chain termination and cytotoxicity
97
What is the main side effect of azathioprine?
Bone marrow suppression
98
What should azathioprine not be prescribed with?
Allopurinol
99
Why should azathioprine not be taken with allopurinol?
Allopurinol deactivates it by transferring a methyl group to it.
100
What is a consequence of TPMT genetic polymorphisms?
Drug toxicity
101
What is essential with long term azathioprine treatment?
Blood tests and monitoring for signs of myelosuppression
102
What class of drug is diclofenac?
Anti-inflammatory / NSAID
103
When is diclofenac prescribed?
Pain Dysmenorrhea Ocular inflammation
104
True or false? Diclofenax is the most favoured non-cox specific NSAID?
False... it's the least favoured
105
What class of drug is celecoxib?
COX-2 specific inhibitor
106
What is celecoxib's mechanism of action?
Preferentially inhibits COX-2 -> reduced prostaglandin production
107
What is a consequence of inhibited prostaglandin synthesis?
Sodium and water retention in ascending loop of Henle
108
What is celecoxib used for clinically?
Rheumatoid arthritis Osteoarthritis Familial adenomatous polyposis
109
What system is potentially negatively affected by celecoxib?
Cardiovascular
110
What type of drug is cyclophosphamide?
Alkylating agent
111
What characteristics do alkylating agents generally have?
Non cell cycle specific | Induce cell death
112
What type of drug is vitamin D?
Steroid
113
How much more affinity does 1,25-dihydroxycholecalciferol have for vitamin D receptors than 25-dihydroxycholecalciferol?
1000
114
What type of drug is cyclosporin?
Immunosuppressive agent
115
What is cyclosporin used for clinically?
Prophylaxis of graft rejection in organ and tissue transplantation
116
What is cyclosporin's mechanism of action?
Binds to cyclophilin, causing inhibition of calcineurin so immunocompetent lymphocytes are inhibited
117
What lymphocytes are preferentially inhibited by cyclosporin?
T lymphocytes
118
What type of drug is aurothiomalate?
Gold based anti-inflammatory
119
What is aurothiomalate used for clinically?
Intramuscular injection
120
What treatments are used as alternatives to aurothiomalate?
DMARDs, biological treatments
121
What type of drug is chloroquine?
Anti-inflammatory agent | Anti-malarial
122
What is chloroquine's mechanism of action?
Inhibits parasitic enzyme heme polymerase -> build cup of toxic heme within parasite
123
How is chloroquine thought to help with rheumatoid arthritis?
Reduces levels of IL6, IL1b and TNF alpha by blocking release or reducing transcription
124
What phase of the cell cycle does methotrexate stop purines/ pyrimidines being incorporated into the DNA?
S phase
125
What type of drug is sulfasalazine?
Immunomodulatory agent
126
What is sulfasalazine used for clinically?
Ulcerative colitis
127
What is the alternative to sulfasalazine?
Mesalazine
128
What is salcatonin?
Calcitonin, hormone produced by thyroid gland
129
What is calcitonin's mechanism of action?
Binds to calcitonin receptor in osteoclasts -> enhancing vit D production -> greater calcium retention -> enhanced bone density
130
Is calcitonin commonly used as a treatment?
No
131
What type of drug is prednisolone?
Glucocorticoid receptor agonist
132
What is prednisolone's mechanism of action?
Crosses cell membrane, binds to corticosteroid receptor -> DNA transcription changes -> reduction of inflammatory proteins
133
What type of drug is raloxifene?
Selective oestrogen receptor modulator
134
What is raloxifene's agonising mechanism of action
Agonisises oestrogen in bone and lipid metabolism Activation of growth factor B3 Inhibits proliferation of preosteoclastic cells
135
What is raloxifene's antagonising mechanism of action?
Antagonises oestrogen in mammary and uterine tissue | Prevents transcriptional activation of genes containing the oestrogen response element.
136
Why is raloxifene not commonly used?
Incidence of hormonal treatment of post-menopausal symptoms is less common
137
What type of drug is alendronic acid?
Nitrogen containing second generation bisphosphonate
138
What is alendronic acid's mechanism of action?
Inhibits FPP synthase by acting as analogues of isoprenoid diphosphate lipids-> reduction in osteoclast activity
139
What is digoxin used for clinically?
Third line for atrial fibrillation
140
Is digoxin used for heart failure?
Rarely, better drugs are available
141
What type of drug is betaxolol?
Beta-adrenergic antagonist
142
What is betaxolol's mechanism of action?
Blocks beta receptors in heart and binds adrenaline and noradrenaline - reduction in heart rate, cardiac output and blood pressure
143
Besides beta receptors in the heart, what can betaxolol block?
Renin release | Beta receptors in the bronchial and vascular smooth muscles
144
True or false? Bisoprolol is a more commonly used beta blocker than betaxolol?
True
145
What is diazepam's mechanism of action?
Binds non specifically to benzodiazepine receptors -> mediation of sleep, muscle relaxation, anticonvulsant activity, motor co-ordination, memory
146
What is diazepam used for clinically?
Anxiety | Muscle relaxant
147
What type of drug is propofol?
Anaesthetic agent
148
What is propofol's mechanism of action?
Inducing increased binding of GABA to GABA-A receptors
149
What is propofol used for clinically?
Intravenous administration for anaesthesia
150
What are the benefits of using propofol?
Produces hypnosis within 40 seconds from start of injection Rapid recovery Associated with less frequent side effects than thiopental and etomidate
151
What type of drug is lamotrigine?
Anticonvulsant
152
What is lamotrigine used for clinically?
Epilepsy | Bipolar disorder
153
What is carbamazepine's believed mechanism of action?
Blocking use-dependent sodium channels | Pain relief to do with blockage of synaptic transmission to trigeminal nucleus
154
What drug do the actions of carbamazepine resemble?
Phenytoin
155
What is carbemazepine used for clinically?
Mood stabiliser in bipolar disorder | First line for trigeminal myalgia
156
What type of drug is phenytoin?
Anticonvulsant
157
What is phenytoin's mechanism of action?
Thought to work in motor cortex, preventing spread of seizure activity
158
What is phenytoin used for clinically?
First line treatment for status eplilepticus
159
What is sodium valproate used for clinically?
Anti-epileptic | Mood stabiliser
160
Of the two drugs which could be used for epilepsy, which is more commonly prescribed: carbamazepine or sodium valproate?
Sodium valproate
161
What is the therapeutic range of sodium valproate?
50-100mcg/mL
162
What type of drug is donepezil?
Reversible acetyl cholinesterase inhibitor
163
What is donepezil's mechanism of action?
Reversible inhibition of acetylcholinesterase
164
What is donepezil used for clinically?
Dementia
165
What type of drug is suxamethonium?
Depolarising skeletal muscle relaxant
166
What is suxamethonium's mechanism of action?
Slower hydrolysis on post synaptic membrane -> prolonged depolarisation -> desensitisation
167
What is suxamethonium used for clinically?
Muscle relaxant after general anaesthetic
168
What type of drug is bromocriptine?
Dopamine agonist
169
What is bromocriptine's mechanism of action?
Stimulates D2 receptor and the Gi signalling cascade -> inhibition of adenyl cyclase, reduction in cAMP and blockage of calcium release
170
What is bromocriptine used for clinically?
Parkinsonian syndrome Hyperprolactinaemia Acromegaly Pulmonary fibrosis
171
Why is bromocriptine used for Parkinsonian syndrome?
Stimulation of D2 receptors in nigrostriatal pathway improves muscle activity and co-ordination
172
Why is bromocriptine less commonly used now?
Concerns about fibrotic reactions | More common to use pramipexole or ropinirole for Parkinson's
173
What type of drug is gabapentin?
Anticonvulsant
174
What is gabapentin's mechanism of action?
GABA analogue Increases synaptic concentration of GABA, enhancing its response Can bind NDMA receptors -> reduced axon excitability
175
What is gabapentin used for clinically?
Neuropathic pain | Adjunct in chronic pain syndromes
176
What type of drug is selegiline?
Dopamine therapy
177
What is selegiline's mechanism of action?
Irreversibly inhibits monoamine oxidase type B (MAO-B) -> enhanced dopamine within nigrostriatal pathways in CNS
178
What is selegiline used for clinically?
Parkinson's | Depression (in higher doses)
179
Why is it that in higher doses, selegiline can be used for Dopamine?
Inhibits Monoamine oxidase-A
180
What is isoflurane used for clinically?
General anaesthetic agent
181
What is isoflurane's mechanism of action?
Induced reduction in junctional conductance Activates calcium dependent ATPase in sarcoplasmic reticulum Binds to GABA, glutamate and glycine receptors
182
What is atracurium's mechanism of action?
Competitively binds to cholinergic receptor sites on motor end plate -> muscle relaxation
183
What drugs can reverse atracurium?
Neostigmine Edrophonium Pyridostigmine
184
What type of drug is memantine?
NMDA antagonist
185
What is memantine's mechanism of action?
binds to NMDA receptor operated channel | Protects against chronically elevated concentrations of glutamate
186
What is memantine used for clinically?
Dementia
187
What type of drug is fentanyl?
Opioid analgesic
188
What is fentanyl's mechanism of action?
Binds to opioid-mu as well as kappa and delta-opioid receptors which are coupled with G proteins Inhibition of nociceptive neurotransmitter release
189
What is fentanyl used for clinically?
IV analgesic Epidurals Transdermal patches for chronic pain
190
What type of drug is paclitaxal?
A microtubule stabilisation agent
191
What is paclitaxal's mechanism of action?
Binds to beta subunit of tubular, causing hyper stabilisation of the microtubule. This stops the cell from functioning properly. Inducing apoptosis in cancer cells by binding to BCL-2
192
What is paclitaxal used for clinically?
Advanced ovarian carcinoma | Breast cancer
193
What is cisplatin's mechanism of action?
Attaches alkyl groups to DNA bases resulting in DNA fragmentation
194
What type of drug is isoniazid?
Bactericidal agent | Prodrug
195
What is isoniazid's mechanism of action?
Targets Mycobacterium | Must be activated by bacterial catalase. Inhibits synthesis of mycologic acids, also disrupts cell metabolism.
196
What type of drug is ethambutol?
Bactericidal agent
197
What are the drugs used to treat tuberculosis?
Rifampicin Isoniazid Pyrazinamide Ethambutol
198
What is ethambutamol's believed mechanism of action?
Inhibits arabinosyl transferases involved in cell wall biosynthesis
199
What type of drug is rifampicin?
Broad spectrum bactericidal
200
What is rifampicin's mechanism of action?
Inhibits DNA-dependent RNA polymerase leading to suppression of RNA synthesis and cell death
201
What is important to note about rifampicin's mechanism of action?
Targets bacterial but not mammalian versions of the enzyme
202
What is pyrazinamide's mechanism of action?
Interferes with FAS I reducing new fatty acid synthesis required for growth and replication Disrupts membrane potential
203
What pH is pyrazinamide's active at?
Slightly acidic
204
What type of drug is ciprofloxacin?
Broad spectrum antibiotic
205
What is ciprofloxacin's mechanism of action?
Inhibits topoisomerase II and IV which are needed for bacterial DNA function
206
What type of drug is budesonide?
Anti-inflammatory corticosteroid
207
What is budesonide used for clinically?
Asthma Crohn's disease Ulcerative colitis
208
What type of drug is montelukast?
Leukotriene receptor antagonist
209
What is montelukast's mechanism of action?
Selectively antagonises leukotriene D4 (LTD4) at the cysteine leukotriene receptor (CysLT1) in the airway
210
What is montelukast used for clinically?
Asthma management Exercise-induced bronchospasm (EIB) Prevents airway oedema, mucus secretion and smooth muscle contraction
211
What kind of drug is ipratropium?
Anticholinergic agent
212
What is ipratropium's mechanism of action?
Non-selectively inhibits muscarinic cholinergic receptors -> decrease in smooth muscle contraction
213
What kind of drug is verapamil?
Class IV anti-arrythmic | Calcium channel blocker
214
What is verapamil's mechanism of action?
Blocks L-type calcium channels -> decreased ionotropy, chronotropy -> reduced heart rate and blood pressure
215
What is verapamil used for clinically?
Hypertension (not common)
216
What type of drug is diltiazem?
Calcium channel blocker
217
What is diltiazem's mechanism of action?
Inhibits influx of extracellular calcium across the myocardial and vascular smooth muscle membranes
218
How do beta-adrenergic antagonists work?
Compete with sympathomimetic neurotransmitters for binding at beta receptors in the heart and its smooth muscle
219
What's the difference between atenolol and propranolol?
Atenolol does not have a negative inotropic effect
220
What is atropine used for clinically?
Heart block
221
What type of drug is glyceryl trinitrate?
Vasodilator
222
What is glyceryl trinitrate's mechanism of action?
Nitroglycerin is converted to nitric oxide (NO), which activates guanylate cyclase, stimulating the synthesis of cGMP, which in turn activates protein kinase G (PKG).
223
What type of drug is amiodarone?
Antianginal Antiarrythmic Class III
224
What is amiodarone's mechanism of action?
Prolongs phase 3 of the myocyte action potential by blocking K+ channels Non-competitive alpha and beta adrenergic inhibitor.
225
What type of drug is adenosine?
Endogenous nucleoside
226
What is adenosine's mechanism of action?
Activates adenosine receptors | Inhibits influx of Ca2+
227
What are the problems with adenosine?
Antagonised by methylxanthines like caffeine and theophylline
228
What type of drug is lidocaine?
Anaesthetic agent
229
What is lidocaine's mechanism of action?
Blocks voltage-sensitive sodium channels during phase 0 of the cardiac action potential-> slowed depressed impulse conduction
230
What is lidocaine used for clinically?
Ventricular arrythmias associated with myocardial infarction
231
What type of drug is losartan?
Angiotensin II receptor blocker
232
What is losartan used for clinically?
Hypertension | Heart failure
233
What is losartan's mechanism of action?
Specifically blocks type-1 angiotensin II receptors which are coupled with G proteins-> reduced blood pressure
234
What type of drug is doxazosin?
Alpha-adrenergic blocking agent
235
What is doxazosin used for clinically?
Hypertension
236
What is doxazosin's mechanism of action?
Selectively inhibits postsynaptic alpha 1 adrenoreceptors on vascular smooth muscle
237
Which drug has doxazosin replaced clinically?
Prazosin
238
What type of drug is spironolactone?
Potassium sparing diuretic
239
What is spironolactone's mechanism of action?
Competitively binds to intracellular aldosterone receptor in DCT cells -> blocking aldosterone actions on gene expression
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What is spironolactone used for clinically?
Hypertension | Chronic heart failure
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What type of drug is chlorpromazine?
Dopamine receptor antagonist Psychotropic agent Sedative Antiemetic
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What is chlorpromazine's mechanism of action?
Antagonises dopaminergic-receptors (subtypes D1, D2, D3 and D4), serotonergic-receptors (5-HT1 and 5-HT2), histaminergic-receptors (H1), alpha1/alpha2-receptors and muscarinic (cholinergic) M1/M2-receptors. Weak presynaptic inhibitor of dopamine reuptake
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What type of drug is allopurinol?
Xanthine oxidase inhibitor
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What is allopurinol's mechanism of action?
Inhibits the enzyme xanthine oxidase-> blocking the conversion of hypoxanthine and xanthine to uric acid decreasing the latter's concentrations.
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What is allopurinol used for clinically?
Prevents gout and renal calculi | Treats uric acid nephropathy, hyperuricemia, and some solid tumours
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What type of drug is diphenoxylate?
Opiate receptor agonist
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What is diphenoxylate used for clinically?
Diarrhoea
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What is diphenoxylate's mechanism of action?
``` Stimulates mu receptors in the GI tract Decreases peristalsis Constricts sphincters Enhances segmentation Prolongs GI transit time ```
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What type of drug is loperamide?
Opiate receptor agonist
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What is loperamide's mechanism of action?
Non-selective calcium channel blocker which also binds to opioid mu-receptors in the myenteric plexus large intestine
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What is loperamide used for clinically?
Acute non-specific diarrhoea | Chronic diarrhoea associated with inflammatory bowel disease
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What type of drug is kaolin?
Adsorption agent Form of aluminium silicate Anti-diarrhoea agent
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What is kaolin's mechanism of action?
Absorbs water Adsorbs toxins and bacteria Overall effect to increase firmness of stool, alleviating fluid loss from diarrhoea
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What type of drug is isphagula husk?
Bulk forming laxative Dietary fibre supplement
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What is isphagula husk used for clinically?
Patients who cannot increase dietary fibre
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What type of drug is lactulose?
Osmotic laxative | Anti-constipation
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What is lactulose's mechanism of action?
Broken down by lactic acid -> increases osmotic pressure -> increased stool water content
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What type of drug is octreotide?
Somatostatin receptor agonist
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What is octreotide's mechanism of action?
Binds to somatostatin receptors -> adenyl cyclase inhibition Stimulation of phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger Via pertussis toxin sensitive G proteins
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What is octreotide used for clinically?
Diarrhoea associated with metastatic carcinoid tumours and vasoactive intestinal peptide secreting adenomas
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What kind of drug is bisacodyl?
Stimulant laxative | Colon cleaner
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What kind of drug is docusate sodium?
Stimulant | Detergent laxative
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What is doscusate sodium used for clinically?
First method to relieve occasional constipation | Helps prevent straining
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What is the mechanism of action for glucocorticoid nuclear hormone receptor agonists?
Bind to cortisol receptors Receptor-ligand complex translocates into the cell nucleus, where it binds to glucocorticoid response elements, causing the increase/decrease in expression of specific target genes
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What is topical hydrocortisone used for clinically?
Treatment of inflammation | Immunosuppresion
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What is betamethasone used for clinically?
In combination with a mineralocorticoid to manage adrenal insufficiency Treatment of inflammation
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What is beclometasone used for clinically?
Steroid-dependent asthma Rhinitis Recurrent nasal polyps
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What type of drug is fludrocortisone?
Mineralocorticoid nuclear hormone receptor agonist
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What is fludrocortisone's mechanism of action?
Binds to mineralocorticoid receptor causing: Increase in ion and water transport Increased extracellular fluid volume and blood pressure Lowering potassium levels
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What is fludrocortisone used for clinically?
Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease Treatment of salt-losing adrenogenital syndrome

Phase I Medicine (46 decks)

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