Drug Names Pharmacology

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Lecture 8: ANS 2 (Acetylcholine)

Hemicholinium: Prevents synthesis of Ach by preventing choline reuptake

Vesamicol: Prevents storage of Ach

4-animopyridine: Enhances release of Ach

Botulinum Toxin (Botox): Prevents release off Ach

Neostigmine: Acetylcholinesterase inhibitor (prolonged Ach in synapse). Useful for treating

myasthenia gravis.

Atropine: Ach antagonist. Used during bradycardia. Increases HR to 80-90 bpm. Also used in

combination with anaesthesia. Bronchodilator. Reduces secretions. Useful for treating gastric hyper

motility.

Pirenzipine: Ach antagonist acting on the M1 receptor. Inhibit gastric acid to treat peptic ulcers.

Bethanechol: helps empty the bladder.

Pilocarpine: Ach agonist. Used to treat glaucoma.

Tropicamide: Ach antagonist. Used for dilating pupils.

Suxamethonium: Neuromuscular blocker acting on nicotinic receptors. Maintains sustained

depolarisation to prevent further generation of Action Potentials. Unaffected by Ach concentrations.

Used during Anaesthesia.

Pancuronium: Competitive antagonist with Ach. Prevents depolarisation.

Lecture 9&10: (Noradrenaline)

Guanethidine: Prevents NA release.

Phenylephrine: α1 agonist on smooth muscle. Vasoconstrictor. Nasal decongestant.

Prazocin: α1 antagonist (alpha blocker). Vasodilator and used for treating hypertension. Can causepostural hypotension and reflex tachycardia.

Clonidine: α2 agonist used to treat hypertension (remember α2 is auto-inhibitory so reduces NA)

Dobutamine: β1 agonist that can increase contractility of the heart. Can lead to a cardiogenic shock

leading to ventricular fibrillation.

Atenolol: β1 agonist

Propanalol: Beta blockers acting on the heart to reduce increased HR, cardiac output, and blood

pressure. Beta blockers can lead to cardiac dysrhythmias.

Salbutamol: β2 agonist Treatment of asthma (bronchodilator). Common to give to patients with

oxygen.



Adrenaline: treatment of anaphylaxis. Β2 agonist

Reserpine: Blocks VMAT. This prevents vesicular storage of NA. More NA remains in synapse and

ends up broken down by MAO. Also reduces serotonin + dopamine levels (VMAT also responsible for

vesicular storage of them) -> could lead to depression.

Amphetamine: displaces NA from the vesicle. Leads to NA being either broken down or cleared out

via diffusion. Amphetamine prevents NA reuptake, enhancing the effects of NA.

Despiramine: prevents reuptake of NA.

Lecture 23:

Suxamethonium: muscle relaxation – Non-competitive ACH antagonist, rapidly hydrolysed by

plasma enterases

Mercaptopurine: S-methylation catalysed by the enzyme thipurine methyl transferase

Perhexiline – anti angina drug. Lack of metabolism leads to neuropathy and hepatotoxicity (liver

toxicity)

Penicillin – common reactions are nausea, vomiting, diarrhoea, and black hairy tongue.

Haemolytic anaemia, leucopoenia, thrombocytopenia. Neuropathy, nephropathy.

Atorvastatin – interacts with drugs. Some increase atorvastatin concentration, while some

interactions increases the other co-administered drug.

Warfarin – narrow therapeutic Index

Ethanol induces an enzyme that bioactivates paracetamol – chronic alcoholics produce more of the

toxic metabolite and risk hepatotoxicity

Lecture 24: Poisons and Antidotes

Absorption:

Ipecac (cephaeline) – vomit inducer. Useful for drugs too big to be removed via lavage. Not suitable

for drugs that will damage the stomach and oesophageal lining upon regurgitation. Not to be used

by N-Acetyl cysteine and Activated charcoal (will just bring it right back up XD)

Activated Charcoal – Decreases absorption. Has greater absorptive properties, out competes the

small intestine in absorption.

Neutralising chemicals:

Deferoxamine – binds to free iron to form Feroxamine. The good useful iron is not affected.

Selective.

N-Acetyl Cystine – Antidote for Paracetamol – neutralises by detoxifying the metabolite or

preventing liver damage via acting as precursor for gluthianone synthesis

Enhance elimination:



Urinary alkalisation via Sodium Bicarbonate – For Aspirin overdose. Aspirin overdose leads to

respiratory alkalosis -> metabolic acidosis

Pharmacodynamic Intervention:

Naloxone – Affects Heroin, antagonist at the receptors that heroin affects. Can cause heroin

withdrawal.

Replace Activity: Vitamin K for excessive Warfarin – treatment period quite long.

Regenerate Target:

Organophosphates – dangerous. Causes SLUDGE + Nicotinic + CNS effects. Inactivates AChE.

Pralidoxime: Treatment starts with Atropine (Antagonise Ach), then this. Removes phosphate gp.

From AChE -> catalytic activity restored.

Lecture 25: Anti-inflammatory

Dexamethasone, prednisone: Steroidal Anti-inflammatory drugs

Aspirin: First line drug for migraine, inhibitor of PG mediated pain, Anti-thrombotic (inhibits TXA2 by

platelets). People with risk of GI ulcers and gastritis are contraindicated.

Paracetamol (acetaminophen): Anti-pyretic + analgesia. Not too useful for anti-inflammatory

conditions. Metabolised into a toxic metabolic, can cause liver damage.

Other non-selective NSAIDs: Ibuprofen, Naproxen, Sulindac, Diclofenac (weak preference for COX-2),Indomethacin.

Lecture 26: Anti-Malarial

Pamaquine: useful for treating p. vivax relapses. Had toxic effect.

Chloroquine: Accumulates in the food vacuole. Interferes with haem digestion. Safe. Resistance is an

issue. Can be used during pregnancy. Need to take for 4 weeks post travel. May exacerbate psoriasis.

Amodiaquine: useful for blood stages of malaria. Unacceptable toxicity.

Primaquine: Treats P. vivax. Works via oxidative stress on parasite. Too toxic – haemolysis and

methaemoglobinamia. G6PD deficiency, pregnancy, and breastfeeding is contraindicated.

Mefloquine (Lariam): Nausea, dizziness. Not recommended if there’s history of epilepsy, psychiatric,

or cardiac conduction abnormalities. Can be used during pregnancy.

Pyronaridine: replacement for chloroquine.

Sulfone/Sulfonamide: inhibit dihydropteroate synthesis. Act too slowly but can be synergistic with

proguanil and pyrimenthamine.

Proguanil: Prodrug. Effective at erthrocytic and liver stages of P. Falciparum. Inhibits DNA synthesis.

Too slow for a cure.



Atovaquone: used in combination with Proguanil in Malarone. Inhibits Electron transport chain, ATP

synthesis, and pyrimidine biosynthesis.

Malarone (proguanil + Atocaquone): Well tolerated med, prophylactic use. Paediatric doses

available. Not suitable during pregnancy, breastfeeding, renal impairment. Expensive

Artemsinin Derivatives: effective, rapid acting, limited toxicity, cheap. Not useful for prophylaxis.

Useful with other drugs to reduce resistance.

Lecture 27: Antibiotics

Penicillin: Bactericidal. Works by inhibiting bacterial cell wall synthesis. Beta Lactam antibiotic.

Chloramphenicol, Tetracycline, Erythromycin (Macrolides), Aminoglycosides: Bacteriostatic.

Inhibition of protein synthesis. Selective toxicity as bacterial ribosome is 70S (as opposed to 80S foreukaryotes)

Cotrimoxazole: Trimethoprim + Sulfonamide. Bacteriostatic. Inhibition of DNA synthesis.

Sulfonamide competes with PABA to inhibit folic acid synthesis. Trimethoprim inhibits DHFR, an

enzyme along the folate synthesis pathway. Less chance of resistance.

Quinolones: Bactericidal. Inhibit DNA synthesis. Inhibit bacterial enzyme DNA gyrase.

Augmentin: contains Amoxicillin + clavulanic acid (Beta lactamase inhibitor)

Lecture 27: Anti-Viral

Zidovudine: NRTI. Prevents RNA -> DNA by terminating the DNA chain. Selective for RT and not DNA

polymerase. Associated with haematological toxicity, pancreatitis, liver damage and severe anaemia.

Nevirapine: NNRTI. Adverse effects include life threatening skin reactions and liver damage.

Saquinavir: Block processing of viral protein. Side effects are nausea, vomiting, diarrhoea.

Enfuvirtide: Fusion Inhibitor. BID SC. Inhibits HIV entry into CD4 cells.

IFN-alpha: treatment for hepatitis C. enhances the immune system and target cells, inhibits viral

replication. TIW SC.

Lecture 28: Anti-Cancer

Side effects of AC drugs: Bone Marrow + immune system suppression. Nausea, vomiting, and

diarrhoea. Oral and GI ulcerations. Alopecia. Teratogenic.

Cyclophosphamide, platinum drugs (CCNS): Alkylating Agents. Transfer alkyl groups to cellular

constituents. Resistance developed by increased production of GSH, increased repair capacity ofDNA damage.



Methotrexate (CCS): Antimetabolite. Inhibit DNA synthesis. Resistance developed by enhanced

expression of alteration of target.

Etoposide (CCS): Topoisomerase Interactive. Induces DNA damage by inhibiting topoisomerase

action

Vincristine: Antimicrotubule. Induce metaphase arrest via disruption of microtubules and mitotic

spindle.

Hormonal Agents: Anti-oestrogen for breast cancer and Anti-androgens for prostate cancer.

Transtuzumab (Herceptin): HER-2 Breast Cancer

Doxorubicin – Anthracycline antibiotics. Resistance by increase expression of P-glycoprotein efflux

pump.

Lecture 30: Anti-hypertensive

Doxazosin: vasoconstrictor antagonist (α-1 adrenoceptor blocker)

Nifedipine: Ca2+ blocker. Vasodilator

Nitric Oxide: vasodilator

Frusemide: Diuretic

Captopril: ACE inhibitor. Leads to vasodilation, Diuresis, and vascular remodelling.

Losartan: Angiotensin II (AT1) receptor antagonist.

Methyldopa: Hypertension during pregnancy (other drugs are contraindicated)

Lecture 34: Anti-DiabeticHumulin: Human Insulin. Prevents hyperglycaemia and ketoacidosis.

Humalog: Fast acting injectable insulin. Treatment for IDDM

NPH/Lente: Intermediate Acting. IDDM.

Ultralente: Long acting. IDDM.

Glargine: Ultra long acting. IDDM

Sulfonylureas: Act on the KATP channels and block them, resulting in depolarisation and influx of

Ca2+. Increase insulin release, and increase insulin sensitivity.

Meglitinides: same mechanism of action as Sulfonylureas except different binding site.

Biguanides & Metformin: stops the liver from making extra sugar when it’s not needed. Can be used

in combination with sulfonylurea drugs.

Drug Names Pharmacology

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