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CEP > Week 2 > Flashcards

Week 2 Flashcards

1
Q

What is pharmacology

A

The study of the mechanism of drug action

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2
Q

What is a drug

A

The active ingredient of a medicine
Any substance which interacts with a biological system and changes it

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3
Q

Which drugs produce their effects not by binding to a receptor but due to their physicochemical properties

A

Antacids
Laxatives
Heavy metal antidotes
Osmotic diuretics
General anaesthetics
Alcohol
Effects are rather non-specific tend to need rather high concentrations

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4
Q

Characteristics of drugs

A

Occur at very low concentrations -high potency
Biological specificity (receptor wise)- molecule and receptor are same however receptors located on different tissues have different effects
Chemical specificity (drug wise)
Stereo selectivity - competition, certain isomer is the active form

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5
Q

How are drugs classified

A

Chemical nature or drug
Symptoms or disease in which they’re used
Organ system affected
Receptor
Duration of action
Generations
Route of administration

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6
Q

What is the receptor concept

A

drugs produce their effects by combining with specific receptor sites in cells
The response is a function of the number of occupied receptors

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7
Q

What is the lock and key hypothesis

A

the shape of the drug complements the shape of the receptor
Chemical specificity
Affinity - the binding ‘strength’ of the drug receptor interaction or the likelihood of binding

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8
Q

What is a drug receptor pharmacology

A

Anything that causes a physiological effect when interacting with a drug is a receptor

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9
Q

Relationship between drug concentration and response

A

Continuous
Saturating . Plateaus
Exhibits threshold
Emax= maximal response
EC50= concentration of agonist which produces half maximal effects
Threshold= required concentration of agonist needed for an initial response
On graph of response against [agonist] shape is HYPERBOLE
On graph of response against log[agonist] shape is SIGMOID
Assumption 1= “response” is ~ concentration of drug receptor complexes
Assumption 2=fixed number of receptors

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10
Q

What’s the difference between EC50 and Kd

A

EC50 is the model-free equivalent of a Kd value
Kd is not the same as EC50, as the point where half receptors are full does not always coincide with point where drugs affect is at 50%

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11
Q

What’s an agonist

A

It binds to a receptor and produce a response
Possess affinity (binding strength) and efficacy (causes effect)

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12
Q

What’s an antagonist

A

Binds to receptors but doesn’t produce a response
Prevent agonist binding and so prevent the response to an agonist
Possess affinity but not efficacy

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13
Q

What is potency

A

A measure of drug activity- a highly potent drug is only required in a very small dose. Hence potency is related to affinity

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14
Q

What is comparative endocrinology

A

Actions of hormones similar throughout evolution
Controlling molecules

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15
Q

What is clinical endocrinology

A

Action of hormones as related to pathology
Controlling molecules

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16
Q

What is the endocrine system

A

A system of ductless glands and cells that secrete hormones
Regulates metabolism, homeostasis and reproduction

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17
Q

What do the endocrine glands do

A

Release secretions into blood directly from cells- ductless glands

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18
Q

What do Exocrine glands do

A

Not part of endocrine system release their secretions outside the body and may be ducted e.g. gut secretions, sweat glands

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19
Q

Mixed glands

A

E.g. pancreas produces digestive juice and insulin, glucagon and somatostatin (growth hormone inhibiting hormone)

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20
Q

Differences between nervous and endocrine system

A

Endocrine has many hormones rather than few neurotransmitters
Endocrine is slower and more long lasting as nervous is generally short lived
Endocrine effect is widespread in blood whereas nervous is localised cell to cell

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21
Q

What is an intracrine signal

A

Generated by a chemical acting within the same cell

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22
Q

What is negative feedback

A

Process by which body senses change and activates mechanism to reduce it
the final product of an endocrine cascade acts to inhibit the release of hormones higher up the cascade

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23
Q

What take the 3 main groups of hormones

A

Protein/peptide
Steroid
Amine

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24
Q

Protein/peptide hormones

A

Made of chains of amino acids
Typically charged
Hydrophilic
Transported in blood without carrier
Preformed and stored in membrane bound vesicles ready for release by exocytosis because hydrophilic they can’t diffuse out

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25
Q

Steroid hormones

A

Act by binding to nuclear receptors
All made from cholesterol (lipid) so hydrophobic can’t travel in blood alone need carriers
Cholesterol to pregnenolone converted to all other steroid hormones by different enzymes
Not stored synthesised as required then diffuse out of cell
Receptors typically in cell primary messengers

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26
Q

Amines/thyroid hormones

A

Tyrosine is an amino acid tyrosine derivatives bound together
T4 contain 4 iodine atoms
T3 contain 3 iodine atoms
Small non polar molecules therefore hydrophobic
Soluble in plasma membrane

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27
Q

The hypothalamus

A

Regulated by hormone-mediated signals and neural inputs
The final common pathway by which signals from multiple systems reach anterior pituitary
Involved in non-endocrine functions e.g. regulation of body temp, thirst, food intake
Sends signals to other parts of nervous system

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28
Q

The pituitary gland

A

Pea sized
Sits in bony cavity at base of brain
Consist of two lobes
Connected to hypothalamus by stalk
Hypothalamus produces hormones directly affecting activity of pituitary

29
Q

Hypothalamus-anterior pituitary hormones

A

GHRH —- GH
Somatostatin inhibits GH
GnRH (gonadotropin releasing hormone)——FSH (follicle stimulating hormone) LH (luteinising hormone )
CRH (Corticotropin releasing hormone) —— ACTH (adrenocorticotrophic hormone)
Thyrotropin releasing hormone (TRH) —— thyroid stimulating hormone (TSH)
Dopamine (inhibits) —— prolactin

30
Q

Growth hormone GH

A

Released throughout life
Stimulated by hypoglycaemia (low blood sugar)
Suppressed by hyperglycaemia (high blood sugar)
Effects mediated by IGF-I
Linear growth in children
Acquisition of bone mass
Stimulates- protein synthesis, lipolysis (fat breakdown), glucose metabolism
Regulation of body composition
Psychological well being

31
Q

Prolactin

A

Essential for lactation
Levels increase dramatically in pregnancy and during breast feeding
Inhibits gonadal activity through central suppression of GnRH (causing decreased LH/FSH)
mainly causes disease when present in excess

32
Q

What’s the function of ACTH

A

Main function is to regulate the glucocorticoid hormone cortisol

33
Q

Function of cortisol

A

Regulates glucose levels
Increases fat in the body
Helps to defend the body against infection
Helps the body respond to stress

34
Q

What does ADH do

A

Polypeptide
Synthesised in supraoptic and paraventricular nuclei of hypothalamus
Secretory granules migrate down the axons of the supraopticohypophyseal tract into the posterior lobe
Causes the kidneys to release less water decreasing the amount of urine produced

35
Q

Oxytocin

A

Stimulates contraction of smooth muscle of breast and uterus
Under positive feedback
Roles in milk ejection reflex, parturition (birth)- synthetic oxytocin can be given to induce labour

36
Q

Major causes of hypopituitarism

A

Pituitary/ parapituitary tumours
Radiotherapy
Pituitary infarction (apoplexy), sheehans syndrome
Infiltration of the pituitary
Trauma
Isolated hypothalamic releasing hormone deficiency

37
Q

GH deficiency

A

Children- poor growth
Adults- increased abdominal fat, decreased lean body mass, impaired lipid profile, decreased muscle strength and exercise capacity, impaired cardiac function, decreased bone mineral density, impaired psychological well being

38
Q

FSH/LH deficiency

A

Children-delayed puberty
Men- decreased libido, impotence, infertility, decreased secondary sex. Decreased muscle mass and strength, mood and well being, osteoporosis, anaemia
Women- decreased libido, menstrual disorders, infertility, dyspareunia, osteoporosis, premature atherosclerosis

39
Q

ACTH deficiency

A

Manifestations- Fatigue, weakness, nausea/vomiting, anorexia, weight loss, hypoglycaemia, hypotension, anaemia

40
Q

TSH deficiency

A

Manifestations- fatigue, weakness, cold intolerance, bradycardia, inability to lose weight, puffiness, pale and dry skin, constipation
Diagnosis- TSH, fT4 and fT3
Treatment- hormone replacement

41
Q

What is central diabetes insipidus

A

Deficient secretion of ADH
Causes- idiopathic, familial, tumours, neurosurgery or trauma, infiltration disorders, infections, hypoxic encephalopathy or severe ischaemia

42
Q

ADH deficiency

A

Manifestations- polyuria, polydipsia, nocturia
Causes of polyuria- DM, renal failure, primary polydipsia, diabetes insipidus

43
Q

What is insulin-like Growth factor 1 IGF-1

A

Hormone that manages the effects of growth hormone in your body
Together IGF-1 and GH promote normal growth of bones of bones and tissues

44
Q

What hormone increases prolactin secretion

A

Thyrotropin-releasing hormone (TRH) stimulates prolactin release

45
Q

What hormone restrains release of prolactin

A

Dopamine inhibits prolactin secretion

46
Q

Hormones secreted by the hypothalamus

A

GH
Vasopressin (ADH)
Adrenocorticotrophic hormone ACTH
Oxytocin
GH releasing hormone GHRH
Gonadotropin releasing hormone GnRH
Corticotropin releasing hormone CRH
Thyrotropin releasing hormone TRH
Follicle stimulating hormone FSH
Thyroid stimulating hormone TSH
Dopamine
LH, somatostatin, insulin-like growth factor 1 IGF-1

47
Q

What is somatostatin

A

Growth hormone inhibiting hormone
Produces predominantly neuroendocrine inhibitory effects across multiple systems
Known to inhibit GI, endocrine, exocrine, pancreatic and pituitary secretions

48
Q

What are physicochemical properties

A

Intrinsic physical and chemical characteristics of a substance
Include appearance, boiling point, density , volatility, water solubility and flammability
Molecular weight, size, partition coefficient, acid dissociation constant and solubility have an impact on pharmacokinetics

49
Q

What type of drug is sodium bicarbonate

A

Antacid- neutralises stomach acid
Acid reflux
Heartburn
Indigestion

50
Q

Examples of laxative drugs

A

Methylcellulose (bulk)- increases amount of water in your stools to help make them softer and easier to pass
Magnesium sulfate (osmotic)- cause water to be retained in the intestinal lumen making stool easier to pass

51
Q

Heavy metal antidotes example

A

EDTA (chelator)
Remove heavy metals such as mercury and lead from blood to stop metal poisoning
Metal poisoning

52
Q

Example of osmotic diuretics

A

Mannitol- given by IV, used to decrease pressure in eyes, as in glaucoma, and to lower intracranial pressure
Filtered in kidneys into the urine drawing water with it causing increased urine production

53
Q

Example of general anaesthetic

A

Halothane

54
Q

Affinity

A

The strength of the drug receptor interaction a potent drug has high affinity

55
Q

Efficacy

A

Refers to ability of a drug-receptor complex to produce a maximum functional response

56
Q

What is a receptor for a hormone endocrinology

A

A bio molecule they have to bind to exert their biological function

57
Q

What is quantitative pharmacology

A

Based on assumption that drugs act by entering into a simple chemical reaction with certain receptors in cells
-simple relation between the amount of drug bound to these receptors and action produced/ size of response

58
Q

What is Kd

A

Dissociation constant
Concentration of ligand which half the ligand binding sites on protein are occupied

59
Q

The Langmuir isotherm

A

A+R<-> AR
Kd= [A]. [R]/[AR]
Rt=total conc receptors
[Rt]= [R] +[AR]
NB: p is the proportion of receptors with agonist bound
P=[AR]/[Rt]
P=[A]/Kd+[A]
Units Kd=mol/litre or M
With the Kd of the drug you can calculate the drugs action quantitatively, Kd only if real binding is according to model if not EC50

60
Q

What are endogenous agonist

A

A compound naturally produced by the body which binds and activates receptor
E.g. acetylcholine, histamine and TNF

61
Q

Exogenous agonist

A

A synthesised drug which binds to a receptor and elicits a response
External factors that bind to various receptors and induce biological a response
For example: synthetic dopamine which binds to dopamine receptor and elicits a response analogous to endogenous dopamine signalling

62
Q

What is meant by recombinant

A

A cell or organism whose genetic material is produced from segments of DNA from different sources joined together-recombinant DNA

63
Q

What is meant by transgenic

A

Genes transferred from one species to another

64
Q

Types of antagonists

A

Competitive
Irreversible/ reversible
Examples:
Atropine -competitive antagonist of ACh, binds to muscarinic receptor to inhibit parasympathetic NS, reversible
Mepyramine (antihistamine)
Etanercept- a decoy receptor that binds to TNF agonist (usually antagonist is a ligand but this is a actual receptor which causes TNF agonist to bind to it and no response occurs)

65
Q

What are beta blockers/ beta-adrenoceptor blocking agents)

A

Class of drugs that prevent stimulation of the adrenergic receptors responsible for increased cardiac action, used to control heart rhythm, treat angina, reduce high blood pressure

66
Q

What’s the difference between an inverse agonist and an antagonist

A

An antagonist binds to receptors preventing agonists from binding and inducing their response
An inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of agonist
A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block activity of either
Both reduce activity of the receptor

67
Q

Example of an inverse agonist

A

Benzodiazepines at GABA receptors

68
Q

State which type of tissue the anterior pituitary is derived from and describe how the posterior pituitary differs from the anterior
What factors are responsible for regulating anterior pituitary hormone production and release

A

Anterior pituitary is made up of glandular tissue. Rathke’s pouch, ectoderm
Posterior pituitary differs in its neuronal origin: derived from the hypothalamus, not glandular but nervous tissue, its largely a collection of axonal projections from hypothalamus. and no hormones are actually made in posterior pituitary
Anterior pituitary hormone production and release is controlled by hypothalamic releasing and inhibiting factors and negative feedback from peripheral hormones

69
Q

Patch clamp technique

A

Used to measure responses generated at receptors
Use a glass pipettes filled with fluid with an electrode in and suck up part of cell, usually one receptor
Then apply electrode to rest of cell generate electric circuit which you can record electric current
Measure electric current, response is now quantifiable current
The binding of an agonist opens the channel
Peaks show that channels open
Partial agonists are less good because they decrease frequency of channel opening

CEP (10 decks)

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