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Pharmacology > Drug Targets + key info > Flashcards

Drug Targets + key info Flashcards

1
Q

What is pharmacodynamics definition

A

Effect of drugs on the body itself

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2
Q

What 2 things are looked at in pharmacodynamics

A

The molecular interactions Drugs have effect on
Eg, effect on target,cell response

Influence of DRUG DOSAGE

Line between toxic and therapeutic

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3
Q

How do we use pharmacodynamics

A

To find suitable dosage and know effect the drug has at good concentration

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4
Q

What is pharmacokinetic definition

A

The effect the body had on the drug

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5
Q

What 4 things are looked at in pharmacokinetics

A

1- absorption or drug into blood stream

2- distribution Eg into ICF of some tissues from the blood

3- metabolism to inactivate the drug

4- excretion of the drug in urine or faeces

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6
Q

Why is pharmacokinetics individual optimal rather than general dosage

A

Peoples metabolism affects how frequently you need to take the drug

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7
Q

Why don’t drugs only treat area applied

A

They are absorbed in blood stream

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8
Q

Drugs can be natural or synthetic. Give example or natural drugs

A

Laxanes from plants for anti cancer

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9
Q

What are the subdivisions of synthetic drugs

A

Completely artificial- codeine

Derived from something in body - insulin engineered

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10
Q

What are drugs which are synthetic but are usually in body called

A

Biologics

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11
Q

What 5 ways do drugs interact with targets / body

A

1- lock and key shape dependent

2- charge / bond dependant

3- hydrophobicity

4- stereochemistry

5- ionisation changes in different ph / pka

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12
Q

How can weak bond / charges between drugs and target affect response

A

It is short term solution drug will unbind

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13
Q

What 4 target proteins for drugs are there

A

Receptors

Ion channels either ligand or voltage

Enzyme

Carrier/channel proteins

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14
Q

What 3 drugs have effect due to chemistry not targets

A

Laxatives - have lactulose which adds water to stool

Antidotes - acetylcysteine stops paracetamol overdose

Antacids - alkaline to neutralise stomach acid

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15
Q

What are agonists and give examples

A

They mimic the action of endogenous chemical messengers

Eg hormones, histamine on H1 receptors, prostaglandins

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16
Q

What are the effects of agonists on the 4 targets

A

Receptors - activated

Ion channels - modulated

Enzymes - activated

Carrier - enhanced

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17
Q

What are antagonists

A

Drugs that inhibit action of agonists and arent endogenous

18
Q

What is the effects on 4 target proteins due to antagonists

A

Receptors - inactive

Ion channels - blocked

Enzymes - inhibited allosterically or non competitively

Carriers - inhibited

19
Q

How is aspirin an example of an agonist NSAID

A

It binds to the enzyme cyclooxgenase irreversibly

Stops prostaglandin production (inflammatory agent)

20
Q

How can benzodiazepines be an agonist

A

It binds to the gaba ligand channel either on the allosteric or Orthosteric site

If it binds to allosteric site as gaba, this increases effect of gaba = more Cl

21
Q

Why is benzodiazepines good for anxiety

A

It causes sleep due to hyperpolarisation of opening Cl channels

22
Q

What is the main example of a receptor drug and explain it

A

SALBUTAMOL

Agonist to the B2 adrenogenic receptor present in lungs

Causes Gs activation and adenylate Cyclase activity

Causes bronchi-dilation for asthma sufferers

23
Q

Give example of an ion channel drug

A

LIDOCAINE ANAESTHETIC

it is an antagonist to the na voltage channel

Causes stop flow of na

No ap = sedation

24
Q

Other than aspirin, give another enzyme target drug

A

Penecillin which is an antagonist to transpeptidase work

Breaks down the cell wall

25
Q

Give an example of a carrier protein targeting drug

A

Omeprazole

which is an antagonist to H pump to stop flow of acid in the stomach to treat ulcers

26
Q

Why are different receptor subtypes important eg the different histamine receptors

A

They have different drugs which can block them at different sites of body to stop drug having multiple effects

27
Q

What do antagonists do to receptor

A

Stop transduction

28
Q

Give an example of a ligand ion channel affected by antagonists

A

Nicotinic ach receptor which if blocked by antagonist stops contraction and ap

29
Q

What 3 subunits does the alpha have in GCRP

A

Gs- stimulating: activates adenylate cyclase or ca channels

Gi- inhibiting : inhibits adenylate cyclase or opens K channels

Gq - activates phospholipase c for Ca2 release

30
Q

Give an example of a GCRP subtype

A

Adrenergic receptors (like salbutamol B2 action)

31
Q

What happens to Alpha 1 adrenergic receptor

A

It has its Gq subunit activated

Activates phospholipase c

Releases ca from sr

Vasoconstriction of muscle

32
Q

What happens to the alpha 2 adrenergic receptor

A

It’s Gi subunit is activated and therefore stops adenylate cyclase activation

No pka activated

Causes no neurotransmitter release

33
Q

What is the B1 adrenergic receptor function

A

It’s Gs is activated

Activates adenylate cyclase

Causes increased HR in the cardiac muscle

(Due to na channels opening) - adenylate cyclase causes NT release

34
Q

What happens when a drug stops usual epinephrine action to increase HR on the alpha 1 adrenergic receptor

A

Epinephrine can’t bind

The alpha 1 receptor doesn’t activate adenylate cyclase

This causes no NT release

No NA channels open

35
Q

What subunit is activated in the B2 adrenergic receptor which salbutamol is agonist to

A

It causes activation of Gs which causes active adenylate cyclase and therefore

Bronchidilation

36
Q

Name 4 enzyme linked receptors

A

Insulin/ RTK
Guanylyl cyclase linked receptor
Serine/threonine kinase receptor
Cytokine receptor

37
Q

WhT are the 2 classes of nuclear/intracellular receptor

A

Class 1- in cytosol and is a homodimer , binds to hormones

Class 2- in nucleus , is a hetereodimer , binds to fatty acids

38
Q

What do receptors have in terms of binding sites

A

Multiple sites drugs binds to

39
Q

How many binding sites do glycine receptors have on ion channel

A

4

40
Q

How many binding sites do nicotinic ach have

A

Homomers have 5

Hetereomers have 2

41
Q

Which sites to competitive drugs bind to eg benzodiazepines on gaba channel

A

Orthosteric to enhance gaba activity

Pharmacology (24 decks)

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