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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
Q

What is cisplatin’s mechanism of action?

A

Attaches alkyl groups to DNA bases resulting in DNA fragmentation, inducing nucleotide mis-pairing and stopping synthesis.

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26
Q

Give an example of a folate antagonist

A

Methotrexate

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27
Q

What is methotrexate’s mechanism of action?

A

Inhibits folic acid reductase which converts folic acid to tetrahydrofolic acid which is needed for DNA synthesis.

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28
Q

How is methotrexate used clinically?

A

Management of severe, active, classical or definite rheumatoid arthritis

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29
Q

What class of drug is phenobarbital?

A

GABA receptor agonist/ barbiturate

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30
Q

What is phenobarbital’s mechanism of action?

A

Acts on GABA receptors to increase synaptic inhibition. This elevates seizure threshold and reduces the spread of seizure activity

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31
Q

What is phenobarbital used for clinically?

A

Management of seizure disorders, excluding absence

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32
Q

What class of drug is pethidine?

A

Opiate receptor agonist

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33
Q

What is pethidine’s mechanism of action?

A

Inhibit adenylate cyclase resulting in a decrease in intracellular cAMP, inhibit nociceptive neurotransmitters, and reduce neuronal excitability.

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34
Q

What class of drug is mannitol?

A

Osmotic diuretic

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35
Q

What is mannitol’s mechanism of action?

A

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.

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36
Q

What class of drug is amphetamine?

A

Non-catecholamine sympathomimetic

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37
Q

What is amphetamine’s mechanism of action?

A

Stimulates the release of noradrenaline and dopamine.
Agonises central 5-HT receptors
Possibly inhibits MAO
Can stimulate peripheral noradrenaline release

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38
Q

What class of drug is warfarin?

A

Vitamin K antagonist

Anticoagulant

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39
Q

What is warfarin’s mechanism of action?

A

Inhibits vitamin K reductase, reducing levels of the reduced form of vitamin K which is needed for the production of coagulation factors

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40
Q

What class of drug is folic acid?

A

Haematinic agent

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41
Q

What is folate’s mechanism of action?

A

Essential for DNA synthesis and cell proliferation, cofactor in synthesis of purines and pyrimidines which are essential in thymidylate synthesis

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42
Q

How is folic acid used clinically?

A

Supplement in pregnancy to avoid spina bifida

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43
Q

What is important to note about the administration of folic acid?

A

It should not be used in undiagnosed megaloblastic anaemias

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44
Q

Why should folic acid not be used in vitamin B12 anaemias?

A

The anaemia may improve but neurological lesions will persist.

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45
Q

What is levonorgestrel used for clinically?

A

Contraceptive

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46
Q

What is levonorgestrel’s mechanism of action?

A

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.

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47
Q

What is a similar drug to Levonorgestrel?

A

Desogestrel

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48
Q

What type of drug is oxytocin?

A

Uterine and lactation stimulant

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49
Q

What is oxytocin’s mechanism of action?

A

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’

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50
Q

What is oxytocin used for clinically?

A

Induction or augmentation of labour when uterine muscle isn’t functioning properly. Used to prevent/ treat haemorrhage postpartum/ due to incomplete abortion.

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51
Q

What type of drug is ethinylestradiol?

A

FSH inhibitor

Contraceptive

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52
Q

What is ethinylestradiol’s mechanism of action?

A

Suppresses the development of the ovarian follicle by inhibiting FSH release from the anterior pituitary.

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53
Q

What is ethinylestradiol used for clinically?

A

Contraception

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54
Q

What class of drug is dinoprostone?

A

Prostaglandin

Uterine stimulant

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55
Q

What is dinoprostone’s mechanism of action?

A

Activates PGF2 receptors on uterine smooth muscle

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56
Q

What is dinoprostone used for clinically?

A

Intravaginal gel used to induce pregnant women by softening and dilating the cervix.

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57
Q

What must be noted before prescribing flucloxacillin?

A

Pneumococci, meningococci and gonococci are all resistant.

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58
Q

What is flucloxacillin’s mechanism of action?

A

Binds to and inhibits the enzyme that cross-links the peptide chain of the building blocks to the peptidoglycan cell wall.

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59
Q

What class of drug is tetracycline?

A

Antibiotic

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60
Q

What is tetracycline’s mechanism of action?

A

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.

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61
Q

Is tetracycline bacteriostatic or bactericidal?

A

Bacteriostatic

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62
Q

What is tetracycline used for clinically?

A

Chlamydia
Ricketts
Brucella
Also effective in infections with mycoplasma and H.influenzae.

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63
Q

What class of drug is gentamicin?

A

Antibiotic

Aminoglycoside

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64
Q

What is gentamicin’s mechanism of action?

A

Causes misreading of mRNA message due to abnormal codon:anticodon recognition

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65
Q

What is gentamicin used for clinically?

A

Meningitis

Septicaemia

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66
Q

What is a major side effect of gentamicin?

A

Ototoxicity (can cause deafness in newborns)

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67
Q

What type of drug is sodium valproate?

A

Anticonvulsant

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68
Q

What is sodium valproate’s mechanism of action?

A

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

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69
Q

What is sodium valproate used for clinically?

A

Treatment and management of seizure disorders, mania and prophylactic treatment of migraine headache

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70
Q

What is ethanol’s mechanism of action?

A

Mimics GABA’s effect in the brain by binding to the respective receptors and inhibiting neuronal signalling

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71
Q

What is ethanol used for clinically?

A

To suppress spasms

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72
Q

What type of drug is cocaine?

A

Indirect sympathomimetic

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73
Q

What is cocaine’s mechanism of action?

A

Inhibits uptake of noradrenaline, leading to its increased effects (notably vasoconstriction)

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74
Q

What is cocaine used for?

A

Local anaesthetic

Widely used drug of addiction

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75
Q

What is a common side effect on cocaine?

A

Necrosis of nasal septum in addicts who snort it.

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76
Q

What type of drug is lithium?

A

Mood stabiliser

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77
Q

What is lithium’s believed mechanism of action?

A

Interferes with membrane ion transport, perhaps including neurotransmitter reuptake

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78
Q

What is lithium used for clinically?

A

Bipolar disorder
Mania
In combination with other agents in unipolar depression

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79
Q

What type of drug is ampicillin?

A

Antibiotic

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80
Q

Is ampicillin bacteriostatic or bactericidal?

A

Bactericidal

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81
Q

What is ampicillin’s mechanism of action?

A

Binds to and inhibits the enzyme that cross links the peptide chain of the building blocks to the peptidoglycan cell wall backbone

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82
Q

Is ampicillin a narrow- or broad-spectrum antibiotic?

A

Broad spectrum

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83
Q

What is important to note about ampicillin administration?

A

Intramuscular
Intravenous
Slow IV infusion

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84
Q

What is the main problem with ampicillin use?

A

It is inactivated by bacterial beta lactamases

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85
Q

Why is clavulanic acid important clinically?

A

It inhibits beta lactamases so is given with ampicillin

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86
Q

What is thalidomide notorious for?

A

Teratogenic effects

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87
Q

What is thalidomide’s believed mechanism of action?

A

May be related to suppression of excessive TNF alpha production

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88
Q

What type of drug is thalidomide?

A

Immunomodulatory agent

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89
Q

What is testosterone used for clinically?

A

Replacement therapy in hypogonadism

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90
Q

What are the side effects of testosterone?

A

Odeoma

Eventual decrease in gonadotropin release -> infertility

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91
Q

What is testosterone’s mechanism of action?

A

Converted to dihydrotestosterone which enters cella and interacts with nuclear receptors to initiate transcription of genes.

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92
Q

What is somatotropin used for clinically?

A

Used to treat dwarfism and growth failure

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93
Q

What is somatotropin’s mechanism of action?

A

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

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94
Q

Is gentamicin bacteriostatic or bactericidal?

A

Bacteriostatic

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95
Q

What type of drug is azathioprine?

A

Purine metabolism antagonist

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96
Q

What is azathiprine’s mechanism of action?

A

Incorporation of thiopurine analogues into the DNA structure -> chain termination and cytotoxicity

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97
Q

What is the main side effect of azathioprine?

A

Bone marrow suppression

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98
Q

What should azathioprine not be prescribed with?

A

Allopurinol

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99
Q

Why should azathioprine not be taken with allopurinol?

A

Allopurinol deactivates it by transferring a methyl group to it.

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100
Q

What is a consequence of TPMT genetic polymorphisms?

A

Drug toxicity

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101
Q

What is essential with long term azathioprine treatment?

A

Blood tests and monitoring for signs of myelosuppression

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102
Q

What class of drug is diclofenac?

A

Anti-inflammatory / NSAID

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103
Q

When is diclofenac prescribed?

A

Pain
Dysmenorrhea
Ocular inflammation

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104
Q

True or false? Diclofenax is the most favoured non-cox specific NSAID?

A

False… it’s the least favoured

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105
Q

What class of drug is celecoxib?

A

COX-2 specific inhibitor

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106
Q

What is celecoxib’s mechanism of action?

A

Preferentially inhibits COX-2 -> reduced prostaglandin production

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107
Q

What is a consequence of inhibited prostaglandin synthesis?

A

Sodium and water retention in ascending loop of Henle

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108
Q

What is celecoxib used for clinically?

A

Rheumatoid arthritis
Osteoarthritis
Familial adenomatous polyposis

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109
Q

What system is potentially negatively affected by celecoxib?

A

Cardiovascular

110
Q

What type of drug is cyclophosphamide?

A

Alkylating agent

111
Q

What characteristics do alkylating agents generally have?

A

Non cell cycle specific

Induce cell death

112
Q

What type of drug is vitamin D?

A

Steroid

113
Q

How much more affinity does 1,25-dihydroxycholecalciferol have for vitamin D receptors than 25-dihydroxycholecalciferol?

A

1000

114
Q

What type of drug is cyclosporin?

A

Immunosuppressive agent

115
Q

What is cyclosporin used for clinically?

A

Prophylaxis of graft rejection in organ and tissue transplantation

116
Q

What is cyclosporin’s mechanism of action?

A

Binds to cyclophilin, causing inhibition of calcineurin so immunocompetent lymphocytes are inhibited

117
Q

What lymphocytes are preferentially inhibited by cyclosporin?

A

T lymphocytes

118
Q

What type of drug is aurothiomalate?

A

Gold based anti-inflammatory

119
Q

What is aurothiomalate used for clinically?

A

Intramuscular injection

120
Q

What treatments are used as alternatives to aurothiomalate?

A

DMARDs, biological treatments

121
Q

What type of drug is chloroquine?

A

Anti-inflammatory agent

Anti-malarial

122
Q

What is chloroquine’s mechanism of action?

A

Inhibits parasitic enzyme heme polymerase -> build cup of toxic heme within parasite

123
Q

How is chloroquine thought to help with rheumatoid arthritis?

A

Reduces levels of IL6, IL1b and TNF alpha by blocking release or reducing transcription

124
Q

What phase of the cell cycle does methotrexate stop purines/ pyrimidines being incorporated into the DNA?

A

S phase

125
Q

What type of drug is sulfasalazine?

A

Immunomodulatory agent

126
Q

What is sulfasalazine used for clinically?

A

Ulcerative colitis

127
Q

What is the alternative to sulfasalazine?

A

Mesalazine

128
Q

What is salcatonin?

A

Calcitonin, hormone produced by thyroid gland

129
Q

What is calcitonin’s mechanism of action?

A

Binds to calcitonin receptor in osteoclasts -> enhancing vit D production -> greater calcium retention -> enhanced bone density

130
Q

Is calcitonin commonly used as a treatment?

A

No

131
Q

What type of drug is prednisolone?

A

Glucocorticoid receptor agonist

132
Q

What is prednisolone’s mechanism of action?

A

Crosses cell membrane, binds to corticosteroid receptor -> DNA transcription changes -> reduction of inflammatory proteins

133
Q

What type of drug is raloxifene?

A

Selective oestrogen receptor modulator

134
Q

What is raloxifene’s agonising mechanism of action

A

Agonisises oestrogen in bone and lipid metabolism
Activation of growth factor B3
Inhibits proliferation of preosteoclastic cells

135
Q

What is raloxifene’s antagonising mechanism of action?

A

Antagonises oestrogen in mammary and uterine tissue

Prevents transcriptional activation of genes containing the oestrogen response element.

136
Q

Why is raloxifene not commonly used?

A

Incidence of hormonal treatment of post-menopausal symptoms is less common

137
Q

What type of drug is alendronic acid?

A

Nitrogen containing second generation bisphosphonate

138
Q

What is alendronic acid’s mechanism of action?

A

Inhibits FPP synthase by acting as analogues of isoprenoid diphosphate lipids-> reduction in osteoclast activity

139
Q

What is digoxin used for clinically?

A

Third line for atrial fibrillation

140
Q

Is digoxin used for heart failure?

A

Rarely, better drugs are available

141
Q

What type of drug is betaxolol?

A

Beta-adrenergic antagonist

142
Q

What is betaxolol’s mechanism of action?

A

Blocks beta receptors in heart and binds adrenaline and noradrenaline - reduction in heart rate, cardiac output and blood pressure

143
Q

Besides beta receptors in the heart, what can betaxolol block?

A

Renin release

Beta receptors in the bronchial and vascular smooth muscles

144
Q

True or false? Bisoprolol is a more commonly used beta blocker than betaxolol?

A

True

145
Q

What is diazepam’s mechanism of action?

A

Binds non specifically to benzodiazepine receptors -> mediation of sleep, muscle relaxation, anticonvulsant activity, motor co-ordination, memory

146
Q

What is diazepam used for clinically?

A

Anxiety

Muscle relaxant

147
Q

What type of drug is propofol?

A

Anaesthetic agent

148
Q

What is propofol’s mechanism of action?

A

Inducing increased binding of GABA to GABA-A receptors

149
Q

What is propofol used for clinically?

A

Intravenous administration for anaesthesia

150
Q

What are the benefits of using propofol?

A

Produces hypnosis within 40 seconds from start of injection
Rapid recovery
Associated with less frequent side effects than thiopental and etomidate

151
Q

What type of drug is lamotrigine?

A

Anticonvulsant

152
Q

What is lamotrigine used for clinically?

A

Epilepsy

Bipolar disorder

153
Q

What is carbamazepine’s believed mechanism of action?

A

Blocking use-dependent sodium channels

Pain relief to do with blockage of synaptic transmission to trigeminal nucleus

154
Q

What drug do the actions of carbamazepine resemble?

A

Phenytoin

155
Q

What is carbemazepine used for clinically?

A

Mood stabiliser in bipolar disorder

First line for trigeminal myalgia

156
Q

What type of drug is phenytoin?

A

Anticonvulsant

157
Q

What is phenytoin’s mechanism of action?

A

Thought to work in motor cortex, preventing spread of seizure activity

158
Q

What is phenytoin used for clinically?

A

First line treatment for status eplilepticus

159
Q

What is sodium valproate used for clinically?

A

Anti-epileptic

Mood stabiliser

160
Q

Of the two drugs which could be used for epilepsy, which is more commonly prescribed: carbamazepine or sodium valproate?

A

Sodium valproate

161
Q

What is the therapeutic range of sodium valproate?

A

50-100mcg/mL

162
Q

What type of drug is donepezil?

A

Reversible acetyl cholinesterase inhibitor

163
Q

What is donepezil’s mechanism of action?

A

Reversible inhibition of acetylcholinesterase

164
Q

What is donepezil used for clinically?

A

Dementia

165
Q

What type of drug is suxamethonium?

A

Depolarising skeletal muscle relaxant

166
Q

What is suxamethonium’s mechanism of action?

A

Slower hydrolysis on post synaptic membrane -> prolonged depolarisation -> desensitisation

167
Q

What is suxamethonium used for clinically?

A

Muscle relaxant after general anaesthetic

168
Q

What type of drug is bromocriptine?

A

Dopamine agonist

169
Q

What is bromocriptine’s mechanism of action?

A

Stimulates D2 receptor and the Gi signalling cascade -> inhibition of adenyl cyclase, reduction in cAMP and blockage of calcium release

170
Q

What is bromocriptine used for clinically?

A

Parkinsonian syndrome
Hyperprolactinaemia
Acromegaly
Pulmonary fibrosis

171
Q

Why is bromocriptine used for Parkinsonian syndrome?

A

Stimulation of D2 receptors in nigrostriatal pathway improves muscle activity and co-ordination

172
Q

Why is bromocriptine less commonly used now?

A

Concerns about fibrotic reactions

More common to use pramipexole or ropinirole for Parkinson’s

173
Q

What type of drug is gabapentin?

A

Anticonvulsant

174
Q

What is gabapentin’s mechanism of action?

A

GABA analogue
Increases synaptic concentration of GABA, enhancing its response
Can bind NDMA receptors -> reduced axon excitability

175
Q

What is gabapentin used for clinically?

A

Neuropathic pain

Adjunct in chronic pain syndromes

176
Q

What type of drug is selegiline?

A

Dopamine therapy

177
Q

What is selegiline’s mechanism of action?

A

Irreversibly inhibits monoamine oxidase type B (MAO-B) -> enhanced dopamine within nigrostriatal pathways in CNS

178
Q

What is selegiline used for clinically?

A

Parkinson’s

Depression (in higher doses)

179
Q

Why is it that in higher doses, selegiline can be used for Dopamine?

A

Inhibits Monoamine oxidase-A

180
Q

What is isoflurane used for clinically?

A

General anaesthetic agent

181
Q

What is isoflurane’s mechanism of action?

A

Induced reduction in junctional conductance
Activates calcium dependent ATPase in sarcoplasmic reticulum
Binds to GABA, glutamate and glycine receptors

182
Q

What is atracurium’s mechanism of action?

A

Competitively binds to cholinergic receptor sites on motor end plate -> muscle relaxation

183
Q

What drugs can reverse atracurium?

A

Neostigmine
Edrophonium
Pyridostigmine

184
Q

What type of drug is memantine?

A

NMDA antagonist

185
Q

What is memantine’s mechanism of action?

A

binds to NMDA receptor operated channel

Protects against chronically elevated concentrations of glutamate

186
Q

What is memantine used for clinically?

A

Dementia

187
Q

What type of drug is fentanyl?

A

Opioid analgesic

188
Q

What is fentanyl’s mechanism of action?

A

Binds to opioid-mu as well as kappa and delta-opioid receptors which are coupled with G proteins
Inhibition of nociceptive neurotransmitter release

189
Q

What is fentanyl used for clinically?

A

IV analgesic
Epidurals
Transdermal patches for chronic pain

190
Q

What type of drug is paclitaxal?

A

A microtubule stabilisation agent

191
Q

What is paclitaxal’s mechanism of action?

A

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
Q

What is paclitaxal used for clinically?

A

Advanced ovarian carcinoma

Breast cancer

193
Q

What is cisplatin’s mechanism of action?

A

Attaches alkyl groups to DNA bases resulting in DNA fragmentation

194
Q

What type of drug is isoniazid?

A

Bactericidal agent

Prodrug

195
Q

What is isoniazid’s mechanism of action?

A

Targets Mycobacterium

Must be activated by bacterial catalase. Inhibits synthesis of mycologic acids, also disrupts cell metabolism.

196
Q

What type of drug is ethambutol?

A

Bactericidal agent

197
Q

What are the drugs used to treat tuberculosis?

A

Rifampicin
Isoniazid
Pyrazinamide
Ethambutol

198
Q

What is ethambutamol’s believed mechanism of action?

A

Inhibits arabinosyl transferases involved in cell wall biosynthesis

199
Q

What type of drug is rifampicin?

A

Broad spectrum bactericidal

200
Q

What is rifampicin’s mechanism of action?

A

Inhibits DNA-dependent RNA polymerase leading to suppression of RNA synthesis and cell death

201
Q

What is important to note about rifampicin’s mechanism of action?

A

Targets bacterial but not mammalian versions of the enzyme

202
Q

What is pyrazinamide’s mechanism of action?

A

Interferes with FAS I reducing new fatty acid synthesis required for growth and replication
Disrupts membrane potential

203
Q

What pH is pyrazinamide’s active at?

A

Slightly acidic

204
Q

What type of drug is ciprofloxacin?

A

Broad spectrum antibiotic

205
Q

What is ciprofloxacin’s mechanism of action?

A

Inhibits topoisomerase II and IV which are needed for bacterial DNA function

206
Q

What type of drug is budesonide?

A

Anti-inflammatory corticosteroid

207
Q

What is budesonide used for clinically?

A

Asthma
Crohn’s disease
Ulcerative colitis

208
Q

What type of drug is montelukast?

A

Leukotriene receptor antagonist

209
Q

What is montelukast’s mechanism of action?

A

Selectively antagonises leukotriene D4 (LTD4) at the cysteine leukotriene receptor (CysLT1) in the airway

210
Q

What is montelukast used for clinically?

A

Asthma management
Exercise-induced bronchospasm (EIB)
Prevents airway oedema, mucus secretion and smooth muscle contraction

211
Q

What kind of drug is ipratropium?

A

Anticholinergic agent

212
Q

What is ipratropium’s mechanism of action?

A

Non-selectively inhibits muscarinic cholinergic receptors -> decrease in smooth muscle contraction

213
Q

What kind of drug is verapamil?

A

Class IV anti-arrythmic

Calcium channel blocker

214
Q

What is verapamil’s mechanism of action?

A

Blocks L-type calcium channels -> decreased ionotropy, chronotropy -> reduced heart rate and blood pressure

215
Q

What is verapamil used for clinically?

A

Hypertension (not common)

216
Q

What type of drug is diltiazem?

A

Calcium channel blocker

217
Q

What is diltiazem’s mechanism of action?

A

Inhibits influx of extracellular calcium across the myocardial and vascular smooth muscle membranes

218
Q

How do beta-adrenergic antagonists work?

A

Compete with sympathomimetic neurotransmitters for binding at beta receptors in the heart and its smooth muscle

219
Q

What’s the difference between atenolol and propranolol?

A

Atenolol does not have a negative inotropic effect

220
Q

What is atropine used for clinically?

A

Heart block

221
Q

What type of drug is glyceryl trinitrate?

A

Vasodilator

222
Q

What is glyceryl trinitrate’s mechanism of action?

A

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
Q

What type of drug is amiodarone?

A

Antianginal
Antiarrythmic
Class III

224
Q

What is amiodarone’s mechanism of action?

A

Prolongs phase 3 of the myocyte action potential by blocking K+ channels
Non-competitive alpha and beta adrenergic inhibitor.

225
Q

What type of drug is adenosine?

A

Endogenous nucleoside

226
Q

What is adenosine’s mechanism of action?

A

Activates adenosine receptors

Inhibits influx of Ca2+

227
Q

What are the problems with adenosine?

A

Antagonised by methylxanthines like caffeine and theophylline

228
Q

What type of drug is lidocaine?

A

Anaesthetic agent

229
Q

What is lidocaine’s mechanism of action?

A

Blocks voltage-sensitive sodium channels during phase 0 of the cardiac action potential-> slowed depressed impulse conduction

230
Q

What is lidocaine used for clinically?

A

Ventricular arrythmias associated with myocardial infarction

231
Q

What type of drug is losartan?

A

Angiotensin II receptor blocker

232
Q

What is losartan used for clinically?

A

Hypertension

Heart failure

233
Q

What is losartan’s mechanism of action?

A

Specifically blocks type-1 angiotensin II receptors which are coupled with G proteins-> reduced blood pressure

234
Q

What type of drug is doxazosin?

A

Alpha-adrenergic blocking agent

235
Q

What is doxazosin used for clinically?

A

Hypertension

236
Q

What is doxazosin’s mechanism of action?

A

Selectively inhibits postsynaptic alpha 1 adrenoreceptors on vascular smooth muscle

237
Q

Which drug has doxazosin replaced clinically?

A

Prazosin

238
Q

What type of drug is spironolactone?

A

Potassium sparing diuretic

239
Q

What is spironolactone’s mechanism of action?

A

Competitively binds to intracellular aldosterone receptor in DCT cells -> blocking aldosterone actions on gene expression

240
Q

What is spironolactone used for clinically?

A

Hypertension

Chronic heart failure

241
Q

What type of drug is chlorpromazine?

A

Dopamine receptor antagonist
Psychotropic agent
Sedative
Antiemetic

242
Q

What is chlorpromazine’s mechanism of action?

A

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

243
Q

What type of drug is allopurinol?

A

Xanthine oxidase inhibitor

244
Q

What is allopurinol’s mechanism of action?

A

Inhibits the enzyme xanthine oxidase-> blocking the conversion of hypoxanthine and xanthine to uric acid decreasing the latter’s concentrations.

245
Q

What is allopurinol used for clinically?

A

Prevents gout and renal calculi

Treats uric acid nephropathy, hyperuricemia, and some solid tumours

246
Q

What type of drug is diphenoxylate?

A

Opiate receptor agonist

247
Q

What is diphenoxylate used for clinically?

A

Diarrhoea

248
Q

What is diphenoxylate’s mechanism of action?

A 
Stimulates mu receptors in the GI tract
Decreases peristalsis 
Constricts sphincters
Enhances segmentation
Prolongs GI transit time
249
Q

What type of drug is loperamide?

A

Opiate receptor agonist

250
Q

What is loperamide’s mechanism of action?

A

Non-selective calcium channel blocker which also binds to opioid mu-receptors in the myenteric plexus large intestine

251
Q

What is loperamide used for clinically?

A

Acute non-specific diarrhoea

Chronic diarrhoea associated with inflammatory bowel disease

252
Q

What type of drug is kaolin?

A

Adsorption agent
Form of aluminium silicate
Anti-diarrhoea agent

253
Q

What is kaolin’s mechanism of action?

A

Absorbs water
Adsorbs toxins and bacteria
Overall effect to increase firmness of stool, alleviating fluid loss from diarrhoea

254
Q

What type of drug is isphagula husk?

A

Bulk forming laxative Dietary fibre supplement

255
Q

What is isphagula husk used for clinically?

A

Patients who cannot increase dietary fibre

256
Q

What type of drug is lactulose?

A

Osmotic laxative

Anti-constipation

257
Q

What is lactulose’s mechanism of action?

A

Broken down by lactic acid -> increases osmotic pressure -> increased stool water content

258
Q

What type of drug is octreotide?

A

Somatostatin receptor agonist

259
Q

What is octreotide’s mechanism of action?

A

Binds to somatostatin receptors -> adenyl cyclase inhibition
Stimulation of phosphotyrosine phosphatase and activation of the Na(+)/H(+) exchanger

Via pertussis toxin sensitive G proteins

260
Q

What is octreotide used for clinically?

A

Diarrhoea associated with metastatic carcinoid tumours and vasoactive intestinal peptide secreting adenomas

261
Q

What kind of drug is bisacodyl?

A

Stimulant laxative

Colon cleaner

262
Q

What kind of drug is docusate sodium?

A

Stimulant

Detergent laxative

263
Q

What is doscusate sodium used for clinically?

A

First method to relieve occasional constipation

Helps prevent straining

264
Q

What is the mechanism of action for glucocorticoid nuclear hormone receptor agonists?

A

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

265
Q

What is topical hydrocortisone used for clinically?

A

Treatment of inflammation

Immunosuppresion

266
Q

What is betamethasone used for clinically?

A

In combination with a mineralocorticoid to manage adrenal insufficiency
Treatment of inflammation

267
Q

What is beclometasone used for clinically?

A

Steroid-dependent asthma
Rhinitis
Recurrent nasal polyps

268
Q

What type of drug is fludrocortisone?

A

Mineralocorticoid nuclear hormone receptor agonist

269
Q

What is fludrocortisone’s mechanism of action?

A

Binds to mineralocorticoid receptor causing:
Increase in ion and water transport
Increased extracellular fluid volume and blood pressure
Lowering potassium levels

270
Q

What is fludrocortisone used for clinically?

A

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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