CA 1

Name the drugs that work on the transporters of the presynaptic cleft

Methylphenidate

Fluoxetine

Cocaine

Amphetamine

MDMA

Name the drugs that work on the vesicles of the presynaptic cleft

Amphetamine

MDMA

How does THC affect the presynaptic cleft

It binds to the CB1 receptor & reduces the frequency of NTs being released into the synaptic cleft

Name the drugs that work on the postsynaptic cleft

Diazepam

Beta Blockers

Adrenaline

Name the drugs that work on the receptors of the postsynaptic cleft

Beta blockers

Adrenaline

Name a beta blocker

Propranolol

Name the drug that works on the ion channels of the postsynaptic cleft

Diazepam

Diazepam is a form of what type of drug

benzodiazepine

Name the receptors that are constitutively active (R*)

Cannabinoid

Benzodiazepine

Serotonin

(other receptors if diseased)

Difference between resistance, tolerance & desensitisation

Resistance = tumours/bacteria adapting to drug

Tolerance = slow adaptation

Desensitisation = fast adaptation

Name 2 phase 1 trials that were pulled & when were they pulled

TGN1412 (Theralizumab) - to treat B cell lymphoma - pulled in 2006

BIA 10-2474 - to treat Parkinson’s Disease - pulled in 2016

Opioid antidote

Nalaxone

Insulin antidote

Glucagon

Paracetamol antidote

N-acetylcysteine (NAC)

Benzodiazepines (e.g. midazolam) antidote

Flumazenil

Heparin antidote

Protamine

Anticholinesterases antidote

Pralidoxime 

Novichok antidote

Atropine

Name 2 NSAIDs, give their function & mechanism

ibuprofen & aspirin (& paracetamol)

Reduce pain, fever & inflammation

Inhibit COX

Role of Statins

Reduce plasma cholesterol

Warfarin role

Anticoaggulant

Clozapine role

Treats treatment resistant schizophrenia

Role of Fluoxetine

(hydrochloride)(brand name = prozac): first successful serotonin reuptake inhibitor, used as an antidepressant

Beta-blockers (e.g. propranolol) role

Prevent β-adrenoceptor-mediated phosphorylation of calcium channels → reduced Ca²⁺ entry → decreased heart contractility.

Role of diazepam

greater hyperpolarisation. works on ion channels of post synaptic neurons (lowers chance of depolarisation)

Role of Glucocorticoids & mechanism

inhibit transcription of COX-2 (cyclo-oxygenase-2), → anti-inflammatory effect.

Name 6 opioids. Of the 6 pick out 2 full opioid agonists & 1 partial

Morphine - full opioid agonist

Heroin - full opioid agonist

Buprenorphine - partial opioid agonist

Codeine - opioid agonist

Fentanyl - opioid agonist

Methadone - opioid agonist

Name a statin & its role & mechanism

Atorvastatin - reduce plasma cholesterol - HMG-CoA reductase inhibitor

Current use of Thalidomide

treatment of leprosy and multiple myeloma

Give 3 examples of Type B drug harm

Anaphylaxis to penicillin

Aplastic anaemia from chloramphenicol

Agranulocytosis from clozapine

ADR with Statins

Muscle pain

ADR with antiepileptic drugs

Teratogenic effect

ADR with Isotretinoin

Teratogenic effect

ADR with Thalidomide

Teratogenic effect - phocomelia (deletion of long bones)

ADR with Sodium valproate

In pregnancy - FVS (foetal valproate syndrome)

ADR with Clozapine

agranulocytosis

ADR with Aspirin

Long term use → gastrointestinal haemorrhage

Why was Cerustatin (Baycol) withdrawn

Why was Thiorazedine withdrawn

Why was Rimonabant withdrawn

4 signs of drug hypersensitivity

Pruritus - itch

Erythematous eruptions - rash

Urticaria - hives

Anaphylactic shock 

What is Anaphylactic shock treated with

Adrenaline, chlorpheniramine, corticosteroid

4 signs of inflammation

Calor (warmth), Rubor (red), Dolor (pain), Tumor (swelling)

What are the 4 types of hypersensitivity, their timing & clinical presentation

What parameters can be derived from a drug/occupancy graph

Bmax

Affinity

Kd

What parameters can be derived from a conc./response graph

Potency

Efficiency

Emax

EC50

What parameters can be derived from a therapeutic/toxic dose graph

TD50

ED50

TI

Origin/Source of morphine

Opium Poppy

Origin/source of codeine

Opium Poppy

Origin/source of THC

Cannabis plant

Origin/source of penicillin

Penicillium mould

When & why was thioridazine withdrawn from the market

Withdrawn in 2005 due to QT prolongation → ventricular arrhythmias

What was the function of rimonabant (Accomplia) and when & why was it withdrawn from the market

Withdrawn in 2008. Was a treatment for obesity but doubled the risk of psychiatric disorder

Why was Cerustatin withdrawn from the market

It is a statin. Withdrawn due to rhabdomyolysis (breakdown of skeletal muscle) & death