Lectures 6-10 Flashcards

1
Q

What would a peak using the patch clamp technique represent?

A

open state receptors

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2
Q

What are inverse agonists?

A

The show affinity but negative efficacy

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3
Q

What are GABA(A) receptors?

A

ligand gated Cl- channels in the brain

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4
Q

What is benzodiazepine?

A

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

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5
Q

What is the significance of Glutamate-gated chloride receptors?

A

They’re common in the nervous system

They’re targeted by anti-parasitic drugs

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6
Q

What are competitive antagonists?

What effect do they have?

A

They bind reversibly at the site of the natural agonist

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

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7
Q

What is important about an SERD’s structure?

A

It reflects oestrogen’s structure

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8
Q

What is fulvestrant?

A

A selective oestrogen receptor degrader

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9
Q

What is the difference between biosimilars and generics?

A

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

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10
Q

Give three examples of drugs that use physio-chemical properties

A

General anaesthetics
Laxatives
Osmotic diuretics

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11
Q

Define drug potency

A

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

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12
Q

What are cardiomyocytes used for?

A

Decreasing blood pressure

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13
Q

What is the therapeutic window?

A

the region between the toxic and effective drug concentrations

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14
Q

What is AVD?

A

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

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15
Q

What is thiopentone

A

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

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16
Q

What are the stages of biotransformation?

A

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

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17
Q

What is a prodrug?

A

A drug with active metabolites

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18
Q

Which drugs are used in clinical trials?

A

those with the maximum potential of reaching the target

19
Q

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

A

paraventricular

supraoptic

20
Q

What hormones are released by the anterior pituitary?

A

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

21
Q

What connects the anterior pituitary to the hyopthalamus?

A

hypothalamic-hypophyseal portal system

22
Q

What connects the posterior pituitary and the hypothalamus?

A

hypothalamic-posterior pituitary stalk

23
Q

What suppresses GH?

A

hyperlgycaemia

24
Q

What does ACTH do?(2)

A

stimulates the production of cortisol by the adrenal cortex

increases ACTH and CTH by positive feedback

25
Q

WHy does testosterone and oestrogen production increase?

A

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

26
Q

What hormones does the posterior pituitary secrete?

A

ADH - regulates blood water potential

Oxytocin - stimulates smooth muscle contraction in breast and uterine tissue

27
Q

What normally causes hypotuitarism?

A

tumours or hormone deficiency

28
Q

What does GH deficiency mean for children?

A

stunted growth

29
Q

What does GH deficiency mean for adults?

A

abdominal obesity and decreased bone density

30
Q

When would GH or testosterone supplements be taken?

A

GH - before bed

Testosterone - in the morning

31
Q

How would you test for ACTH deficiency?

A

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

32
Q

How is ACTH deficiency treated?

A

homrone replacement therapy (hyrdocortisone is metabolised into cortisol)

33
Q

How is TSH deficiency presented?

A

Brachycardia

Skin irritation

34
Q

What might cause polyuria?

A

Polydipsia
Renal failure
ADH deficiency

35
Q

What is acromegaly?

A

GH hypersecretion usually caused by a pituitary adenoma

36
Q

What is cushing’s syndrome?

A

corticotroph adenoma

37
Q

What is the agonist for GABA(A)

A

diazepam

38
Q

What is the antagonist for GABA(A)

A

flumanzenil

39
Q

define absorption

A

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

40
Q

How would ion trapping move weak acids?

A

they would move from acidic environments to basic environments

41
Q

What are modified release tablets?

A

They have a membrane that is selectively permeable to water

42
Q

What is transit time?

A

absorption time availability

43
Q

What are the 3 different types of drug administration?

A

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