Core Drugs Flashcards by Zaheerah Mohammed

Example of a ligand-gated ion channel

Nicotinic ACh receptor

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Example of a G protein-coupled receptor

Muscarinic ACh receptor

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Example of a kinase-linked receptor

Cytokine receptors

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Example of a nuclear receptor

Oestrogen receptor

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Nicotinic acetylcholine receptors

Permeable to Na+, K+, Ca2+
Nonspecific cation channel
Expressed on the post-ganglionic neuronal cell in ANS

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Describe neurotransmission (events at the synapse)

Action potential travels down the presynaptic neuron —> calcium influx
NTs carried in vesicles until they fuse with the membrane of presynaptic neuron —> released into synapse
NTs bind to receptors on postsynaptic neuron until threshold is reached
Excitation, action potential

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Drugs that act as agonists at Nicotinic ACh receptors

Acetylcholine (full)
Nicotine (full)
Varenicline (partial - good sub for nicotine withdrawal)

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What binds and activates adrenoreceptors

Adrenaline and noradrenaline

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Example of a G-protein coupled receptor

Adrenoceptors

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Adrenaline binding to a1 adrenoceptor

Vasoconstriction
Gq - activation of phospholipase C

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Adrenaline binding to a2-adrenoceptor

Relaxation of GI tract
Presynaptic inhibition of noradrenaline in CNS
Gi - inhibition of adenylyl cyclase

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Adrenaline binding to B1-adrenoceptor

Increased HR and cardiac muscle contraction
Gs - stimulation of adenylyl cyclase, increased cAMP)

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Adrenaline binding to B2-adrenoceptor

Bronchodilation
Increased HR and cardiac muscle contraction
Gs - stimulation of adenylyl cyclase, increased cAMP)

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Adrenaline binding to B3-adrenoceptor

Thermogenesis in skeletal muscle, lipolysis
Gs - stimulation of adenylyl cyclase, increased cAMP)

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Adrenaline

Binds to ALL adrenoceptors

Full sympathetic physiological response

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Isoprenaline

Binds to B1 and B2 adrenoceptors

Tachycardia and bronchodilation

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Salbutamol

Binds to B2 adrenoceptors

Bronchodilation
Treats acute symptoms of asthma

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Theophylline

Phosphodiesterase inhibitor (terminates action of cAMP)

Indicated for COPD

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Example of a kinase-linked/enzyme-coupled receptor agonist

Insulin

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Signalling cascade effects activated by insulin receptor

Recruitment of glucose transporters
Increased formation of glycogen
Increased formation of fat
Changes in gene expression
Decreased glycogen to glucose conversion
Increased formation of protein

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What are Nuclear receptors

Intracellular receptors (located in nucleus) bound by steroid hormones
Hormone-receptor complex binds to DNA and affects gene transcription

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What binds to nuclear receptors

Steroid hormones

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Steroid hormones are …. and pass through plasma membrane to bind to …

Hydrophobic/lipophilic

Nuclear receptors

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Receptor: androgen
Ligand:

Testosterone

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Receptor : oestrogen Ligand:

17beta- oestradiol

Receptor: glucocorticoid Ligand:

Cortisol, corticosterone

Receptor: progesterone mineralocorticoid Ligand:

Progesterone

Receptor: aldosterone receptor Ligand:

Aldosterone

Aldosterone is secreted in response to …

Hyponatremia (low Na+ in blood) - causes resistance to thiazides

Thiazides

A type of diuretic — reduce fluid build-up in the body (lowers BP)

Condition: hypokalaemia

Low K+ levels in blood

Drug targets can be divided into 4 main categories:

Receptors Enzymes Ion channels Carrier proteins

What is ibuprofen

An anti-inflammatory drug

Indication for ibuprofen

Pain and inflammation in rheumatic disease and musculoskeletal disorders

Mechanism of action for ibuprofen

Decreases blood flow by inhibition of prostaglandins (usually causes vasodilation)

Pharmacokinetics of ibuprofen

Half life = 1.2 - 2hrs Liver disfunction = 3.1-3.4hrs

Side effects of ibuprofen

Irritation of GI tract Impairment of renal function

What is amlodipine

Calcium channel blocker

Indication of amlodipine

Angina and hypertension

Pharmacokinetics of amlodipine

Long half life (40hrs) Over 50hrs if renal disfunction

Side effects of amlodipine

Reduction in arterial BP Reduction in smooth muscle contraction NOT SUITABLE FOR EMERGENCY

What are selective serotonin re-uptake inhibitors (SSRIs) indicated for

Depression Antagonist binds (blocks) serotonin receptors. More serotonin at synapse

Symptoms of SSRIs

MANY Anxiety, weight changes, headache, arrhythmias, constipation, nausea etc…

Examples of SSRIs

Citalopram Escitalopram Fluoxetine Fluvoxamine Paroxetine Sertraline

Sodium valproate

Treats epilepsy and bipolar disorder

Amitriptyline

(Tricyclic) Antidepressant

Side effects of amitriptyline

Sedation (H1 receptor blockage) Dry mouth and constipation (mACh receptor blockage)

Pindolol

Treats hypertension Partial agonist, Beta-blocker Indicated for ventricular tachycardias, atrial fibrillation

Isoprenaline and propranolol bind to …..

The same B1-adrenoceptor

What does propranolol do

- Blocks adrenaline - Activation of B1 results in reduction of HR and force of contraction - Can also bind to B2 - t1/2 = 8hrs

Why does propranolol cause pharmacodynamic drug interaction

- Also has affinity for B2, blocks action of salbutamol —> exacerbate symptoms for asthmatic patients —> reduce effect of salbutamol

Aspirin

Anti-platelet drug (blood thinner) - Prevents blood clotting Also used as a painkiller Irreversible competitive antagonist

Atenolol

Beta-blocker used to treat angina and high BP Low lipid solubility

Codeine

Used to relieve acute moderate pain More basic than acidic

Paracetamol

Painkiller and used to treat fever

Bisoprolol

Beta blocker selective for B1 Treats hypertension, angina and heart failure

Dihydropyridine calcium channel blockers and examples

Decrease SVR and ABP amlodipine and nicardipine

Nicardipine

Angina and hypertension

Digoxin

Arterial fibrillation + flutter, heart failure

Isosorbide dinitrate

Prophylaxis and angina

What are flecainide and propafenone examples of and indicated for

Sodium channel blockers Arrhythmias

Amiodarone

Arrhythmias Potassium channel blocker

What do calcium channel blockers do

Decrease myocardial contractility + electrical impulses

Examples of non-dihydropyridine and it’s indication

Verapamil, diltiazem Prophylaxis + angina

ACE inhibitors function, indication, and name examples

Inhibit angiotensin I —> angiotensin II Heart failure, hypertension Ramipril, lisinopril, perindopril

Angiotensin receptor antagonist examples and indications

Losartan, candesartan, irbesartan Hypertension

Beta blocker examples

Bisoprolol Atenolol Propranolol Metoprolol Carvedilol Sotalol

Metoprolol

Hypertension treatment

Carvedilol

Hypertension treatment

Sotalol

Arrhythmias + arterial fibrillation

Example of loop diuretics and their indications

Furosemide, bumetanide Oedema

Examples of thiazide/thiazide like diuretics

Bendroflumethiazide, indapamide, chlorthalidone

Bendroflumethiazide

Oedema

Indapamide

Hypertension

Chlorthalidone

Oedema, hypertension, heart failure

Warfarin

Anticoagulant - “blood thinner” Prophylaxis and treatment of venous thrombosis and pulmonary embolism

Heparin

Anticoagulant - “blood thinner” pulmonary embolism, unstable angina, DVT

Lidocaine

Arrhythmias, anaesthesia (nerve block) Related to cocaine

Gaviscon and peptac are examples of … used for …

Antacids Gastro-oesophageal reflux

Types of laxatives and their use

Bulk, osmotic, stimulant Constipation

Loperamide

Diarrhoea, pain of bowel colic in palliative care

Proton pump inhibitor (PPI) examples and indications

Lansoprazole, omeprazole, prantoprazole GI ulcer prevention/treatment, gastro-oesophageal reflux

Cimetidine

H2 receptor antagonist GI ulcer prevention/treatment, gastro-oesophageal reflux

Gliclazide

Type 2 diabetes

Insulin

Type 1 and type 2 diabetes

Metformin

Type 1 and type 2 diabetes

Macrolides examples and indications

Clarithromycin, erythromycin Penicillin alternative (antibiotic)

Penicillin examples

Amoxicillin, benzylpenicillin

Clotrimazole

Fungal/vaginal infections