Lectures 6-10

Question 1

What would a peak using the patch clamp technique represent?

Answer 1

open state receptors

Question 2

What are inverse agonists?

Answer 2

The show affinity but negative efficacy

Question 3

What are GABA(A) receptors?

Answer 3

ligand gated Cl- channels in the brain

Question 4

What is benzodiazepine?

Answer 4

GABA(A) agonist
It increases the affinity of the GABA binding site for GABA
It hence increases openings

Question 5

What is the significance of Glutamate-gated chloride receptors?

Answer 5

They’re common in the nervous system

They’re targeted by anti-parasitic drugs

Question 6

What are competitive antagonists?

What effect do they have?

Answer 6

They bind reversibly at the site of the natural agonist

They produce a parallel shift to the right of the agonist dose

Question 7

What is important about an SERD’s structure?

Answer 7

It reflects oestrogen’s structure

Question 8

What is fulvestrant?

Answer 8

A selective oestrogen receptor degrader

Question 9

What is the difference between biosimilars and generics?

Answer 9

Biosimilars are modelled after drugs using living organisms, where generics are synthetic drugs

Question 10

Give three examples of drugs that use physio-chemical properties

Answer 10

General anaesthetics
Laxatives
Osmotic diuretics

Question 11

Define drug potency

Answer 11

drug activity expressed in terms of the amount required to produce an effect of given intensity

Question 12

What are cardiomyocytes used for?

Answer 12

Decreasing blood pressure

Question 13

What is the therapeutic window?

Answer 13

the region between the toxic and effective drug concentrations

Question 14

What is AVD?

Answer 14

Apparent Volume of Distribution
The volume of fluid to dilute the absorbed dose to the concentration found in plasma
AVD = dose/[plasma]

Question 15

What is thiopentone

Answer 15

A short acting barbiturate, causing unconsciousness within 30-40 seconds

Question 16

What are the stages of biotransformation?

Answer 16

1 - oxidation using cytochrome p450 transmembrane enzymes in the ER to form -OH groups
2 - conjugation (forms small soluble molecules)

Question 17

What is a prodrug?

Answer 17

A drug with active metabolites

Question 18

Which drugs are used in clinical trials?

Answer 18

those with the maximum potential of reaching the target

Question 19

What are the names of the nuclei of the hypothalamus regulating posterior pituitary function?

Answer 19

paraventricular

supraoptic

Question 20

What hormones are released by the anterior pituitary?

Answer 20

Growth hormone (GHRH)
FSH/LH (Gonadotropin RH)
Adenocorticotropic homrone (corticotropin RH)
Thyroid stimulating hormone (thyrotropin releasing hormone)
Prolactin

Question 21

What connects the anterior pituitary to the hyopthalamus?

Answer 21

hypothalamic-hypophyseal portal system

Question 22

What connects the posterior pituitary and the hypothalamus?

Answer 22

hypothalamic-posterior pituitary stalk

Question 23

What suppresses GH?

Answer 23

hyperlgycaemia

Question 24

What does ACTH do?(2)

Answer 24

stimulates the production of cortisol by the adrenal cortex

increases ACTH and CTH by positive feedback

Question 25

WHy does testosterone and oestrogen production increase?

Answer 25

decreased sensitivity to them (as negative feedback would increase their production)

Question 26

What hormones does the posterior pituitary secrete?

Answer 26

ADH - regulates blood water potential | Oxytocin - stimulates smooth muscle contraction in breast and uterine tissue

Question 27

What normally causes hypotuitarism?

Answer 27

tumours or hormone deficiency

Question 28

What does GH deficiency mean for children?

Answer 28

stunted growth

Question 29

What does GH deficiency mean for adults?

Answer 29

abdominal obesity and decreased bone density

Question 30

When would GH or testosterone supplements be taken?

Answer 30

GH - before bed | Testosterone - in the morning

Question 31

How would you test for ACTH deficiency?

Answer 31

Short Synacthen testing insulin test glucagon test (hypoglycaemia is a key presentation)

Question 32

How is ACTH deficiency treated?

Answer 32

homrone replacement therapy (hyrdocortisone is metabolised into cortisol)

Question 33

How is TSH deficiency presented?

Answer 33

Brachycardia | Skin irritation

Question 34

What might cause polyuria?

Answer 34

Polydipsia Renal failure ADH deficiency

Question 35

What is acromegaly?

Answer 35

GH hypersecretion usually caused by a pituitary adenoma

Question 36

What is cushing's syndrome?

Answer 36

corticotroph adenoma

Question 37

What is the agonist for GABA(A)

Answer 37

diazepam

Question 38

What is the antagonist for GABA(A)

Answer 38

flumanzenil

Question 39

define absorption

Answer 39

the movement of a drug from its site of administration to the plasma

Question 40

How would ion trapping move weak acids?

Answer 40

they would move from acidic environments to basic environments

Question 41

What are modified release tablets?

Answer 41

They have a membrane that is selectively permeable to water

Question 42

What is transit time?

Answer 42

absorption time availability

Question 43

What are the 3 different types of drug administration?

Answer 43

Enteral (oral/rectal) Parenteral (subcutaneous - IV) Percutaneous (inhalation)