Pharmacology Flashcards

1
Q

Pharmacodynamics is?

A

How the drug affects the body

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2
Q

4 types of cellular receptors

A

Ligand gated ion channels
G-protein coupled receptors
Enzyme linked receptors
Intracellular receptors

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3
Q

What is a ligand gated ion channel

A

Channel that opens briefly when a specific ligand binds to it

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4
Q

How is a G protein coupled receptor activated

A

Ligand binds to outside of cell
GTP replaces the GDP attached to the alpha unit (inside the cell)
Alpha unit detaches and causes response

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5
Q

How many subunits in a G-protein receptor

A

3

alpha, beta, gamma

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6
Q

What is the final intracellular messenger from activating a G-protein receptor?

A

cAMP

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7
Q

How many enzyme linked receptors have to be activated to produce a response?

A

2

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8
Q

When 2 enzyme-linked receptors bind together, what is the result

A

They aggregate, form a dimer and then convert ADP to ATP

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9
Q

Tyrosine kinase is a common example of which receptor type?

A

Enzyme linked receptor

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10
Q

Describe the path a ligand takes to activate an intracellular receptor

A

Passes through cell membrane
Binds to receptor
Moves into nucleus
Causes synthesis of specific proteins

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11
Q

What is EC50?

A

The dose required to produce 50% of the maximum pharmacological effect

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12
Q

Is a higher or lower EC50 more potent?

A

Lower EC50 is more potent

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13
Q

What is Emax

A

Maximum efficacy of the drug

All receptors are occupied by the drug

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14
Q

What happens to a dose response curve with a competitive antagonist?

A

Shift it to the right

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15
Q

3 types of antagonist?

A

Competitive, irreversible covalent and allosteric

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16
Q

What happens to dose response curve with irreversible antagonist?

A

Moves it down, i.e. reducing the maximal efficacy

17
Q

How does the dose response curve change with allosteric antagonists?

A

It shifts it to the right

18
Q

How do you calculate therapeutic index?

A

Dose of that drug that causes toxicity in 50% of the population (TD50)
divided by
dose of that drug that causes therapeutic change in 50% of the population (ED50)

19
Q

What is pharmacokinetics

A

What the body does to the drug

20
Q

What are the 4 steps in pharmacokinetics?

A
ADME
absorption
distribution
metabolism
elimination
21
Q

4 methods of absorption

A

Passive diffusion
Facilitated diffusion
Active transport
Endocytosis

22
Q

Passive diffusion is what?

A

Drug moves through membrane down a concentration gradient

23
Q

What is facilitated diffusion?

A

Drug moves across membrane through specific membrane channels

24
Q

What is active transport?

A

ATPase membrane protein moves drug against concentration gradient

25
Q

What is endocytosis?

A

Cell membrane engulfing large molecules

26
Q

What is bioavailability?

A

How much drug makes it into the blood

Area under curve of oral drug divided by area under curve for IV drug multiplied by 100

27
Q

What is first order kinetics?

A

The drug is eliminated a certain % at a time and the concentration graph becomes a curve

28
Q

What is zero order kinetics?

A

Rate of elimination is constant, concentration graph becomes a decreasing straight line

29
Q

What is the steady state concentration?

A

After a certain number of doses, the elimination and absorbing of the drug becomes equal, the aim is to achieve this within the therapeutic range

30
Q

What type of drugs are less easily excreted by the kidney?

A

Lipid soluble

31
Q

What process happens to lipid soluble drugs before they can be excreted by the kidneys?

A

Transforming them into water soluble chemicals, through 2 reactions: phase 1 and phase 2

32
Q

3 types of phase 1 reactions?

A

oxidation
hydrolysis
reduction

33
Q

phase 2 reactions do what?

A

addition of a polar group

34
Q

Name 6 cytochrome P450 inhibitors (PCRABS)

A
Phenytoin
Carbamazepine
Rifampicin
Alcohol
Barbiturates
St John's wort
35
Q

Name some cytochrome P450 inhibitors (G-PACMAN))

A
Grapefruit
Protease inhibitors
Azole antifungals
Cimetidine
Macrolides (except azithromycin)
Amiodarone
Non-DHP CCB's (diltiazem and verapamil)
36
Q

Name 4 common adverse effects of opiods

A

Constipation
Nausea/vomiting
Sedation
Dry mouth

37
Q

Common dose of opiod to be given for breakthrough pain?

A

1/6th of the total 24h dose to be given PRN no more often than 2 hourly

38
Q

Name 5 anti-emetics

A
haloperidol
levomepromazine
metoclopramide
domperidone
ondansetron
ciclizine