Pharmacology- Drugs and Therapeutics Flashcards

1
Q

What is a drug?

A

A chemical with a selective therapeutic action

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2
Q

What is pharmacology?

A

Science that deals with the study of drugs and their actions on living systems

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3
Q

What are the TWO integral branches of pharmacology?

A

Pharmocodynamics- What the drug does to the body- Drug action and mechanisms

Pharmocokinetics- What the body does to the drug- ADME

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4
Q

What does the Adrenergic receptor- beta (B-1) do?

A
  1. Increases heart rate
  2. Increases cardiac muscle’s force of contraction

This is the adrenaline effect on the heart

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5
Q

What does the adrenergic receptor- beta (B-2) do?

A
  1. Relaxes the airway
  2. Dilates smooth muscles

This is the adrenaline effect on the lungs

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6
Q

What is biological specficity in therapeutic action

A

Right target

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7
Q

What is chemical specifcity in therapeutic action

A

Right target binding site

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8
Q

What is biolgical specficity in adverse/side effects?

A

Non-specific binding site

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9
Q

What is chemical specificity in adverse/side effects?

A

Non-specific binding site

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10
Q

What is specificity?

A

Target binding sites (receptors and its subtypes) provides the selectivity for the specific binding of drugs/ligands (Lock and Key system)

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11
Q

What are the key drug binding sites?

A
  1. Drugs as enzyme inhibitors- blocks the enzyme activity
  2. Drugs as enzyme substrates
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12
Q

Give examples of drugs and their enzymes and how they block the process.

Drugs as enzyme inhibitors

A
  1. Sildenafil- targets the phosphodisterase enzyme and it blocks the
    enzyme, which function is intracellular breakdown
  2. Neostigmine- enzyme is Acetylcholine esterase and it will inhibit neurotransmitter degradation
  3. Ibuprofen (reversible), Aspirin (irreversible)- enzyme is cyclo-oxygenase and its function is messenger synthesis.

So the medication blocks that enzyme and then that will block the enzyme function/activity

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13
Q

Which out of aspirin and ibuprofen binds to an enzyme and is reversible and which is irreversible?

A

Aspirin- irreversible
Ibuprofen- reversible

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14
Q

What is reversible antagonists?

A

Readily dissociate from their receptor

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15
Q

What is irreversible antagonists?

A

Form a stable, permanent or nearly permanent chemical bond with their receptor.

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16
Q

What is pseudo-irreversible antagonists?

A

Slowly dissociate from their receptor

17
Q

Give an example of drugs as enzyme substrates

A

Dopamine- enzyme acting as a substrate.
E.g. dopamine precurosor L-DOPA for parkinson’s disease

18
Q

What is competitive binding?

A

Drug competes for the ligand active site. Can be reversible and irreversible

19
Q

Example of competitive inhibitor

A

Neostigmine (medication) is a comeptitive inhibitor with Acetylcholine which comeptes to bind with the Acetylcholine esterase

20
Q

During competitive binding neostigmine will compete with _____ to bind to the ligand active site of Acetylcholine (Ach) esterase?

A

Acetylcholine

21
Q

What is non competitive binding?

A

Drug binds at different site. Irreversible

22
Q

Example of non competitive binding

A

Cycloxygenase enzyme (COX) is responsible for the synthesis and release of prostaglandins (a pro-inflammatory cytokine). The synthesis of prostaglandin required arachidonic acid.

The arachidonic acid binds to the COX enzyme and releases the prostaglandins.

Example
Aspirin binds to the COX and it will not allow the arachidonic acid binding to the COX.

23
Q

The 3 class of drug targets

A
  1. Enzymes
  2. Drugs targeting transporters
  3. Drugs targeting voltage-gated ion channels
  4. Drugs targeting receptors
24
Q

Cocaine mechanism

A

Blocking of the transporter reducing the uptake of noradrenaline constant stimulation

25
Q

Drugs targeting transporters

A

The transporter is a protein, most of the drugs acting on the transporters are inhibitors. They block the transport

26
Q

Example of drugs targeting voltage gated ion channels

A

Its a trans membrane channel, its not a receptor because it doesn’t require binding of drug. It just recognizes the membrane potential. They have specific sensors to detect the inside, outside electric environment.
Once the channels open, it allows the ions to mobilise so its exclusively for ion movement. Inward/outward of ions. Could be Na, K, Ca, F ions (depending on which ion channel). The fastest

27
Q

Example of drug targeting ion channel

A

Lidocaine which is a local anesthetic. Blocks the Sodium (Na) channel.

28
Q

What are drugs targeting receptors?

A

proteins which respond to a endogenous messenger by initiating a signal
could be hormones, peptides, cytokines, neutrotrasnmitters etc

29
Q

What are the key types of receptors?

A
  1. Nuclear receptors
  2. Ligand gated ion channels
  3. Catalytic receptors
  4. G-protein coupled receptors
30
Q

Benefits vs risk (market authorisation of clinical drugs

A

Thalomid- treatment used to treat nausea in pregnant woman, caused birth defects

31
Q

Aspirin

A

Therapeutic action- COX inhibitor, anti-inflammatory (fever, pain, blood thinner)
Adverse effects- gastric upset, bleeding and ulcer. If given to children under 12, causes reyes syndrome which is liver and brain damage