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Cardiovascular, renal and PNS > Drugs > Flashcards

Drugs Flashcards

1
Q

Trimetaphan

A

Ganglionic blocker (blocks transmission of Ach)

used for CVS (lowers BP) + hypertension

[side effects]
-Tachycardia
-Reduced secretions
-Pupil dilation
-Sexual dysfunction

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2
Q

Metirosine

A

Inhibits initial enzyme (tyrosine hydroxylase) in synthesis of NA

Possible use in catecholamine-secreting tumour

[side effects]

-Headaches
-Heavy sweating
-Tachycardia
-High BP
-Pale face/being sick
-Anxious/panick

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3
Q

Cardidopa

A

Inhibits synthesis of DOPA to dopamine DOPA decarboxylase

Parkinson’s disease
- reduces metabolism in periphery = reduced sympathetic effects of levodopa (high BP and racing heart)
-doesn’t cross BBB (increases levodopa availability in CNS)

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4
Q

methyldopa (Aldomet)

A

Metabolised to methyl-NA = false precursor molecule

A2 agonist

Inhibits DOPA decarboxylase

Treat pregnancy-induced hypertension andd pre-eclampsia

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5
Q

Guanethidine

A

Transported via same mechanism as NA

Blocks adrenergic neurons that releases NA

[side effects]
Bradycardia
Digestive disorders
Nasal congestion
Sexual dysfunction

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6
Q

Reserpine

A

Inhibits VMAT -> prevents transport of NA into vesicles (vesicular levels fall)

hypertension treatment

[side effects]
- hypotension
- bradycardia
- digestive disorders
- nasal congestion
- sexual dysfunction

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7
Q

phenylephrine

A

Selective alpha-1 agonist

used as …
- Decongestant
- Pupil dilation
- Increase BP
- Relieve hemorrhoids

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8
Q

clonidine

A

Selective alpha-2 agonist

Prevents NA release

Reduces BP – treat hypertension

[side effects]
- Drowsiness
- Oedema

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9
Q

isoprenaline

A

beta agonist

asthma treatment

[side effects]
- tachycardia
- dysthymia

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10
Q

dobutamine

A

Beta-1 agonist

Treats cardiogenic shock + severe heart failure by increases cardiac contractility

[side effects]
Dysrhythmia

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11
Q

Salbutamol

A

Selective beta-2 agonist

Treats asthma by relaxing smooth muscle

[side effects]
- Tachycardia
- Dysrhythmia
- Tremor

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12
Q

Clenbuterol

A

Beta-2 agonist

Treats chronic breathing disorders (e.g. asthma) -> bronchodilator

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13
Q

mirabegron

A

beta-3 agonist

treats overactive bladder syndrome

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14
Q

amphetamine

A

Indirect acting sympathetic agonists

Reverses NET and VMAT
= NA release from vesicles

Narcolepsy
Obesity
ADHD

[side effects]
- Hypertension
- Tachycardia
- Insomnia
- Psychosis
- Dependence

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15
Q

ephedrine

A

beta agonist

causes NA release

used as a decongestant

[side effects]
- Hypertension
- Tachycardia
- Insomnia
- Psychosis
- Dependence

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16
Q

cocaine

A

blocks NET = synaptic NA release

[side effects]
- hypertension
- abuse / dependence

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17
Q

phenoxybenzamine

A

Alpha-antagonist
NET inhibitor

[side effects]
- hypotension
- tachycardia
- nasal congestion

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18
Q

phentolamine

A

alpha antagonist

[side effects]
- hypotension
- tachycardia
- nasal congestion

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19
Q

Prazosin, tamsulosin, doxazosin

A

Alpha-1-antagonist

treats:
- hypertension
- prostatic hyperplasia (prostate enlargement)

[side effects]
- ejaculation failure

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20
Q

Yohimbine

A

alpha-2 antagonist

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21
Q

labetalol

A

Alpha/beta antagonist

Hypertension in pregnancy

[side effects]
Bronchoconstriction
Postural hypotension

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22
Q

carvediol

A

alpha/beta antagonist

treats heart failure and hypertension

[side effects]
-Bronchoconstriction
-Postural hypotension
-renal failure

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23
Q

propranolol

A

beta antagonist

treats:
- angina
- hypertension
- cardiac dysrhythmia
- glaucoma

[side effects]
-Bronchoconstriction
-Cardiac failure
-Cold extremities
-Fatigue
-Depression
-Hypoglycaemia

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24
Q

atenolol

A

beta-1-antagonist

treats angina, hypertension and dysthymias

[side effects]
-Bronchoconstriction
-Cardiac failure
-Cold extremities
-Fatigue
-Depression
-Hypoglycaemia

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25
Q

timolol

A

beta-1-antagonist

treats glaucoma

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26
Q

methacholine

A

Muscarinic and nicotinic agonist

Bronchial provocation test

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27
Q

bethanechol

A

Muscarinic and nicotinic agonist – via M3

treats bladder hypotonia

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28
Q

atropine

A

Non-selective competitive muscarinic antagonist

treats:
-CNS depression/excitation
-anticholinesterase poisoning
-GI hypermotility (anti-spasm)
- lazy eye (has long-lasting mydriasis effect; put on good eye to blur vision and strengthen weak eye)

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29
Q

hyoscine (scopolamine)

A

Non-selective competitive muscarinic antagonist

TREATS:

GI relaxant (treat bowel pain)

CNS depression/excitation

Sedating

Motion sickness - blocks transmission from vestibular apparatus to vomiting centre

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30
Q

Pirenzepine

A

M1 selective antagonist – inhibits vagus-induced histamine release (no direct effect on smooth muscle)

treats peptic ulcers

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31
Q

Darifenacin, oxybutynin & tolterodine

A

M3 selective antagonists

Inhibits involuntary bladder contraction and micturition

[side effects]
- dry mouth
- blurred vision
- constipation

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32
Q

Iptatropium

A

Quaternary ammonium compound

TREATS:
- Irritant induced bronchospasm
-Asthma
-bronchitis
-COPD

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33
Q

Curare / d-tubocurarine

A

Non-depolarising agent

binds to nicotinic receptor at NMJ as an antagonist

blocks neuromuscular nerve transmission but not nerve conduction/muscle contractility

causes paralysis

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34
Q

Alpha-bungarotoxin

A

Irreversible binding to nACh receptors at NMJ

Inhibits post-synaptic Ach binding

SIDE EFFECTS:

Hypotension - due to ganglionic blockade

Histamine release from mast cells

Bronchospasm in sensitive individuals

Respiratory failure - assisted ventilation used

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35
Q

Gallamine / pancuronium

A

M2 blockade (blocks Ach transmission/binding)

used as anaesthetic

side effects:
- tachycardia

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36
Q

Suxamethonium

A

mimicks Ach at neuromuscular junction

hydrolysis = much slower so depolarisation is prolonged = neuromuscular blockage

USES:

  1. Intubation – paralyses larynx
  2. Surgery during pregnancy/caesarean
    - Doesn’t cross BBB
    - Doesn’t affect newborn respiration
  3. Electroconvulsive therapy
  4. Lethal injection

SIDE EFFECTS:
- Bradycardia
- Potassium release + hyperkalemia (increase in permeability at end plate -> net loss of K+)
- Post-operative pain
- Increased intraocular pressure
- Prolonged paralysis

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37
Q

Neostingmine

A

Acetylcholinesterase inhibitor

Raises Ach in synapse

Quaternary ammonium compound -> competes with Ach

USES:
Reverses non-depolarising block at end of anaesthesia

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38
Q

Sugammadex

A

Chelates amino-steroid non-depolarising blockers

Avoids use of cholinesterase inhibitors/depolarising agents

USES:
Reverses non-depolarising block at end of anaesthesia

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39
Q

Tropicamide

A

Non-selective muscarinic antagonist -> causes pupil dilation

Used for ocular examination

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40
Q

Dipivefrin

A

Adrenoceptor agonists (due to lipophilicity, it penetrates anterior chamber of eye more easily than epinephrine)

reduces AH production

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41
Q

Brimonidine

A

Alpha-2 adrenoceptor agonist

treats glaucoma by reducing AH formation

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42
Q

Brinzolamide

A

Carbonic anhydrase inhibitor

Decreases intracellular bicarbonate (required for AH formation)

Treats glaucoma

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43
Q

Carbachol; Pilocarpine

A

Miotics - Muscarinic agonists

Improves drainage of AH through trabecular network

Treats glaucoma and dry eyes

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44
Q

Latanoprost

A

PGF2α analogue

Improves drainage through uveoscleral outflow

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45
Q

Verteporfin

A

Used in combination with photodynamic therapy

treats wet AMD

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46
Q

Pegatanib

A

VEGB binding molecule

BV growth/leak stimulated by vascular endothelial growth factor (VEGF)

treats wet AMD

47
Q

Lifitegrast

A

integrin αLβ2 antagonist (immune inhibiting)

treats dry eyes

Blocks inflammation which can limit tear fluid production

48
Q

Sodium cromoglycate

A

mast cell stabiliser

treats allergies in eye

49
Q

Hemicholinium

A

Competitive inhibitor of choline uptake

Blocks reuptake of choline by high-affinity choline transporter

= inhibition of Ach synthesis

50
Q

Vesamicol

A

Blocks Ach transport on synaptic vesicles

Acts pre-synaptically

= inhibition of Ach transport

51
Q

Triethylcholine

A

False transmitter – no depolarising actions

Acetylated to form acetyltriethylcholine (ATC)

52
Q

Tetradotoxin

A

blocks voltage-gated Na+ channels (no depolarisation along motor nerve)

causes muscular paralysis + respiratory failure

53
Q

Mg2+ streptomycin + neomycin

A

Blocks Ca2+ channels (no Ca2+ influx)

54
Q

Botulinum toxin

A

Type of protease that is transported into nerve terminals + cleaves SNARE proteins required for vesicle fusion + release Parasympathetic + motor paralysis for months

USED FOR:

  1. Botox
  2. Persistent eye/neck spasms
  3. Crossed eyes
  4. Cerebral palsy
  5. Excessive sweating
  6. Migraines

SIDE EFFECTS:

Dry mouth
Blurred vision
Difficulty swallowing
Respiratory paralysis

55
Q

Alpha-bungarotoxin + beta-bungarotoxin

A

Irreversibly binds to nACh receptors at NMJ

Inhibits post-synaptic acetylcholine binding
Acts on pre-synaptic motor nerve terminals to block release of Ach

Has phospholipase PLA2 activity = destruction of nerve terminal

56
Q

delta-atracotoxin

A

Prolongs Na+ channel opening + AP
= nerve firing stimulation

57
Q

edrophonium

A

Short-acting anti-cholinesterase

Forms ionic bond with AchE at anionic site

58
Q

Neostigmine; physostigmine; pyridostigmine

A

Medium-duration anti-cholinesterase

Competitive inhibitor at anionic + esteric sites

Carbamylate-enzyme complex is much slower to hydrolyse

treats myasthenia gravis

59
Q

Dyflos; sarin; novichok

A

Irreversible anti-cholinesterase

Used as war-gases + pesticides

60
Q

Pralidoxime

A

Rescue for irreversible AChE inhibitor
Reactivates enzyme by bringing oxime group into close proximity with phosphorylated enzyme

= strong nucleophile + attracts phosphate groups from serine-OH

Strips organophosphate from enzyme

61
Q

Fampridine

A

Blocks neuronal K+ channels

Increases Ach release at NMJ

treats multiple sclerosis - improves motor function

SIDE EFFECTS:
- increased muscle spasms

62
Q

ivabradine

A

directly blocks funny current

used to treat heart failure + angina

SIDE EFFECTS:
- AV block
- visual disorders

63
Q

Disopyramide; procainamide; quinidine

A

Class I anti-arrhythmic drugs

64
Q

Lidocaine

A

Class I anti-arrhythmic drug

SIDE EFFECTS:
- drowsiness
- disorientation
- convulsions
- respiratory depression

65
Q

Flecainide; Propafenone

A

Class I anti-arrhythmic drugs

can cause sudden death in patients with MI

66
Q

esmolol

A

short-acting beta-1 selective blocker

67
Q

Amiodarone

A

[class III]

Blocks Na+ and Ca2+ channels

Decreases expression of β1-adrenoceptors

TREATS:
- Arrythmias
- Thyroid abnormalities
- Corneal deposits
- Pulmonary disorders
- Skin pigmentation

68
Q

Sotalol

A

Non-selective beta-blocker

69
Q

Verapamil

A

Class IV Phenylalkylamine

Slows down HR + reduces cardiac contractibility

SIDE EFFECTS:
- constipation
- hypertension

70
Q

Diltiazem

A

Class IV Benzothiazepine

Slows down HR + reduces cardiac contractibility

SIDE EFFECTS:
- constipation
- hypertension

71
Q

digoxin

A

Cardiac glycoside

Increases intracellular Na+ = increase in contractility

TREATS:
- atrial fibrillation or flutter
- Heart failure

SIDE EFFECTS:
- Cardiac toxicity
- Gastric irritations
- diarrhea
- Nausea
- Vomiting
- Yellow/blurred vision
- Headache
- Bradycardia

72
Q

Levosimendan

A

Calcium sensitiser

Binds to tropomyosin C to prolong action

short-term treatment for heart failure

73
Q

Acetalzolamide

A

Carbonic anhydrase inhibitor

Decrease in Na+ reabsorption

Weak diuretic

can cause mild acidosis (proton retention) and urine alkalosis (due to bicarbonate secretion)

74
Q

Mannitol

A

Osmotic diuretic

Decreases water reabsorption

Increases Na+ excretion by retaining diluted filtrate

Acts on part of nephron freely permeable to water
- PCT
- Descending loop of Henle
- Collecting tubule

TREATS:

Weak diuretic

Cerebral oedema – decreases intracranial pressure

Glaucoma – reduces intraocular pressure

75
Q

Hydrochlorothiazide; Bendroflumethiazide

A

[thiazide drugs]

Reduce Na+ / Cl- reabsorption

TREATS:
- hypertension
- mild heart failure
- severe resistant oedema
- prevents kidney stone formation (reduces Ca2+ excretion into renal tubules)

SIDE EFFECTS:
- Tachyarrythmias
- Hyperglycemia
- Increased cardiac toxicity of digoxin

76
Q

Chlortalidone; indapamide; metalazone

A

[thiazide-like drugs]

Reduce Na+ / Cl- reabsorption

TREATS:
- hypertension
- mild heart failure
- severe resistant oedema
- prevents kidney stone formation (reduces Ca2+ excretion into renal tubules)
-hypertension

SIDE EFFECTS:
- Tachyarrythmias
- Hyperglycemia
- Increased cardiac toxicity of digoxin

77
Q

Spironolactone (active drug = canrenone) ; epleronone

A

Mineralcorticoid (aldosterone) receptor antagonist (MRAs)

inhibits effect of aldosterone

treats heart failure

78
Q

Amiloride ; triameterene

A

Renal Na+ channel (ENaC) blocker

Inhibits effect of aldosterone

treats chronic heart failure (if associated with angina)

79
Q

Captopril

A

ACEI (short-acting)

SIDE EFFECTS:
- metallic taste/loss of taste
- skin rash
- tachycardia
- hyperkalaemia

80
Q

Enalapril

A

ACEI (long-acting)

SIDE EFFECTS:
- metallic taste/loss of taste
- skin rash
- tachycardia
- hyperkalaemia

81
Q

Losartan; valsartan

A

ARBs

82
Q

Aliskiren

A

Renin inhibitor

SIDE EFFECTS:
- in pregnancy -> teratogenic effect

83
Q

Nifedipine; Amlodipine

A

Calcium channel blocker

treats hypertension -> causes arterial dilation (decreases TPR and cardiac afterload)

SIDE EFFECTS
- postural hypotension (decreased ability of arteries to constrict rapidly when person is standing up)
- Tachycardia
- Headache and flushes
- Constipation

84
Q

Minoxidil

A

anti-hypertensive drug

SIDE EFFECTS
- hirsutism (excessive hair growth)

85
Q

Hydralazine

A

Treats hypertension in pregnancy + heart failure in patients of African-American origin

SIDE EFFECTS
- lupus-like symptoms
- tachycardia
- peripheral oedema

86
Q

Nebivolol

A

Beta-1 selective beta-blocker

Stimulates NO release in vascular endothelium

causes vasodilation (less fatigue/bradycardia)

87
Q

Pindolol

A

Beta-1 selective beta-blocker

88
Q

Moxonidine

A

Alpha-2 / imidazoline receptor agonist

treats resistant hypertension

SIDE EFFECTS:
- dry mouth
- sedation/drowsiness

89
Q

Evolocumab

A

PCDK9 inhibitor

treats atherosclerosis

90
Q

Ezetimibe

A

Cholesterol absorption inhibitor

treats atherosclerosis

91
Q

Glyceryl trinitrate (GTN)

A

Organic nitrate vasodilator (Short-acting)

treats angina

SIDE EFFECTS
- hypotension
- reflex tachycardia
- headache
- dizziness

92
Q

Isosorbide dinitrate / mononitrate

A

Organic nitrate vasodilator (long-acting)

treats angina

SIDE EFFECTS
- hypotension
- reflex tachycardia
- headache
- dizziness

93
Q

Nicorandil

A

Activates vascular ATP-sensitive potassium channels

Angina – causes venodilation (decreases cardiac preload) and arteriodilation

SIDE EFFECTS
- dizziness
- headaches
- tachycardia
- ulcerations on skin, eye and GI

94
Q

Ranolazine

A

Inhibits late sodium current (which is activated by ischaemia in cardiac mayocytes)

Prevents Ca2+ overload (leads to contraction)

treats angina

95
Q

aspirin

A

Binds to COX-1 and COX-2, preventing conversion of arachidonic acid to PGH2

anti-platelet agent

SIDE EFFECTS:
- GI bleeding
- bronchospasms
- hypersensitivity

96
Q

Ticlopidine; Clopidogrel

A

P2Y12 antagonist (irreversible)

1st generation thienopyridine

Anti-platelet agent

SIDE EFFECTS:
- Dyspepsia
- Diarrhoea
- Rashes
- Neutropenia

97
Q

Prasugrel

A

P2Y12 antagonist (irreversible)

2nd generation thienopyridine

anti-platelet agent

SIDE EFFECTS:
- rashes

98
Q

Ticagrelor

A

P2Y12 antagonist (reversible, non-competitive allosteric inhibitor)

Cyclopentyl-triazolo-pyrimidine derivative

anti-platelet agent

99
Q

Cangrelor

A

P2Y12 antagonist (Reversible, competitive, high affinity inhibitor)

ATP analogue

anti-platelet agent

100
Q

Abciximab

A

Glycoprotein IIb/IIIa receptor inhibitor

chimeric mAB

anti-platelet agent

101
Q

Eptifibatide

A

Glycoprotein IIb/IIIa receptor inhibitor

Synthetic cyclic heptapeptide

anti-platelet agent

102
Q

Tirofiban

A

Glycoprotein IIb/IIIa receptor inhibitor (competitive reversible inhibitor)

Synthetic non-peptide agent

anti-platelet agent

103
Q

Dypyridamole

A

Phosphodiesterase inhibitor

Anti-platelet agent + causes vasodilation

104
Q

heparin

A

Binds to antithrombin III, which accelerates inactivation of thrombin, factor Xa and factor Ixa

105
Q

Protamine sulfate

A

Polycationic, highly positively charged protein derived from salmon sperm protein

4500Da

Binds to negatively charged UFH to form stable, inactive ion pairs

Antidote for anticoagulant action -> reverse bleeding

SIDE EFFECTS:
- hypersensitivity
- less reactive against LMWHs

106
Q

Fondaparinux

A

Factor Xa inhibitor

Synthetic pentasaccharide anticoagulant

Mimics unique binding sequence of heparin to ATIII + enhances interaction with active site of factor Xa

anticoagulant

no antidote

107
Q

Apixaban; rivaroxaban

A

Factor Xa inhibitor

Blocks conversion of prothrombin to thrombin (anticoagulant)

Novel oral anticoagulant (NOAXs)

Antidote = andexanet alka (modified recombinant factor Xa)

108
Q

Hirudin, lepirudin & bivalrudin

A

Direct thrombin inhibitors – binds and inhibits only free form of active thrombin (IIa)

anticoagulant

109
Q

Dabigatran

A

Direct thrombin inhibitor

Inhibits both free and fibrin-bound forms of thrombin

Antidote = idarucizumab (humanised mAB fragment)

anticoagulant

110
Q

warfarin

A

Blocks vitamin K epoxide reducatase enzyme, which uses vitamin K to produce clotting factors

oral coagulant

SIDE EFFECTS:
- osteoporosis
- teratogenicity

111
Q

Alteplase; streptokinase + urokinase

A

Fibrinolytic agent – converts plasminogen to plasmin

treats acute MI, thrombotic stroke & thromboembolism

112
Q

Teranexamic acid

A

Fibrinolytic agent

Synthetic derivative of lysine

Competitive inhibition of plasminogen activation by blocking lysine binding sites on plasminogen

Blocks plasmin non-competitively at high conc.

TREATS:
- Haemorrhage complications associated with thrombolytic surgery
- patients at high risk of pre/post operative haemorrhage
- Heavy menstrual bleeding

SIDE EFFECTS:
- nausea
- vomiting
- diarrhoea

113
Q

Milrinone

A

Phosphodiesterase type 3 inhibitor (PDE3)

Inhibits degradation of cAMP (= increases its conc. )

TREATMENT FOR CHF:
- Increases cardiac output
- Reduces right arterial pressure (less risk of pulmonary oedema)
- Reduces TPR (due to peripheral arterial/venous dilation)

Cardiovascular, renal and PNS (16 decks)

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