FOP resit paper past paper 1

First-pass metabolism occurs after which route of drug administration:

oral

Salbutamol is used in the treatment of asthma because it is:

β₂-adrenoceptor agonist

Phase II clinical trials involve:

testing the treatment of patients who are ill

nitric oxide

activates soluble guanylyl cyclase in smooth muscle

acts via intracellular receptors?

Hydrocortisone

Which GABAA agonist is used as a sedative

Benzodiazepines

Activation of adenylyl cyclase results in the production of which signalling molecule(s) inside the cell?

cyclic adenosine monophosphate (cAMP)

The objective of the lead optimisation phase of drug development is to:

check for unwanted effects in animals, pharmacokinetic analysis

Which of the following are true regarding treatments targeting serotonin?

Serotonin reuptake inhibitors increase serotonin in synapses      5-HT₃ antagonists are used to prevent chemotherapy-induced nausea, 5-HT₁ agonists are used in migraine therapy

Which of the following is/are physiological actions of cortisol?

increased blood glucose levels

increased breakdown of body protein stores

decreased cellular uptake of glucose

Acetylcholine produces:

bradycardia by stimulating M₂ muscarinic receptors on the sinoatrial cells

bronchial smooth muscle constriction via M₃ muscarinic receptors vasodilation by stimulating M₃ muscarinic receptors on endothelial cells

M3 Receptor activation in the eye cause:

Allow drainage of aqueous humour

  Constriction of the pupil

Describe the steps involved in the pre-clinical phase of drug development (10 marks) first 2 bullet points

• Candidate molecules chosen: target identification (e.g. proteins target; G-proteins).

• Target validation, mention techniques used in the lab

Describe the steps involved in the pre-clinical phase of drug development (10 marks) second 2 bullet points

• Lead Identification and optimisation; high through put screening; invertebrate models

• In vivo animal models

Describe the steps involved in the pre-clinical phase of drug development (10 marks) third 2 bullet points

• Toxicity testing, pharmacokinetic analysis, formulation - suitable formulations and dosage forms devised

• Mention Legislation and 3Rs and alernatives method examples:

  • In vitro methods: cell culture; organotypic assays; organ on a chip

Computer based models

• Invertebrate Models: drosophila; c. elegans

Describe the functional effects of one GABA and one glutamate blocker and their clinical uses. (10 marks) GABA Blocker: e.g. Bicuculline (Flumazenil)

GABA Blocker: e.g. Bicuculline (Flumazenil)

This is a competitive GABA-A receptor antagonist. Acts at the benzodiazepine binding site. Increases neuronal excitability by removing the potentiation of Cl⁻ conductance that benzodiazepines produce. It is used clinically to reversal the effects of benzodiazepine overdose, restoring consciousness and respiratory drive. It is also used to reverse benzodiazepine sedation following anaesthesia.

Describe the functional effects of one GABA and one glutamate blocker and their     clinical uses. (10 marks) Glutamate Blocker: e.g Ketamine

This is a NMDA receptor non-competitive antagonist, a ligand-gated ion channel activated by glutamate. Acts as open-channel blocker, entering channel pore, preventing Ca²⁺ and Na⁺ influx. Reduces excitatory postsynaptic signalling throughout the CNS. Results in dissociative anaesthetic state i.e. profound analgesia, sedation, and amnesia. Leaves airway reflexes and respiratory drive intact. Clinically, used in anaesthesia induction, and can also be used for acute and chronic pain management at lower doses