Pharmacodynamics Flashcards

1
Q

What is the definition of pharmacodynamics?

A

It is the branch of pharmacology attributed to the molecular, biochemical, and physiological effects of drugs.

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2
Q

Define affinity.

A

How well a drug molecule binds to a receptor site.

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3
Q

Define specificity.

A

The ability of a drug to produce an action at the desired site (and not anywhere else).

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4
Q

Define efficacy.

A

The ability of a drug to produce at effect.

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5
Q

Define potency.

A

The relative amount of a drug required to produce the desired effect.

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6
Q

Define ligands.

A

Ions/atoms/molecules that bind to receptor sites.

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7
Q

Define endogenous.

A

Originating from inside [the body/organism/cell].

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8
Q

Define exogenous.

A

Originating from outside [the body/organism/cell].

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9
Q

Define agonists and antagonists.

A

Agonists effect protein function.

Antagonists block their function.

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10
Q

What are receptors made up of?

A

Receptors are usually made up of protein molecules.

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11
Q

Where are receptors found in the cell?

A

Receptors are found on the cell surface, spanning the membrane and in the cytoplasm.

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12
Q

Define the process of receptor conformation (shape changing).

A

Confirmation occurred when a receptor is exposed to certain environmental conditions and/or ligands (e.g. pH, temperature, signalling molecules).

Ligands bind at the molecular binding site and conformation results in enzyme/catalyst activation or deactivation - initiating an intracelular response.

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13
Q

What are some examples of agonist drugs?

A

. Salbutamol - Activates B2 receptors expressed by pulmonary, skeletal and cardiac muscle cells.

. Morphine - Targets MOR opioid receptors expressed by cells in the CNS and GI.

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14
Q

What is an example of a commonly used antagonist drug?

A

Naloxone - Binds to MOR opioid receptor sites without activating an intracellular response. (Blocks MOR, preventing morphine taking effect).

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15
Q

What is the purpose of membrane transport proteins?

A

Facilitates movement of molecules and ions unable to diffuse through the cell membrane.

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16
Q

How do membrane transport proteins allow movement of molecules and ions?

A

They change shape in response to stimuli allowing movements in and out of the cell.

Channel proteins allow movement from high to low concentrations only.

Most common types and ligand-gated and voltage-gated.

17
Q

What are some examples of drugs that target transport proteins?

A

. Amiodarone - Inhibits the Na-K pump, resulting in slower repolarisation of cardiac muscle cells. (Extends the QT segment).

. Diazepam - Binds to GABAa receptors (ligand-gated CI- channel) decreasing neurone action potentials.

18
Q

What are enzymes and what is their function?

A

They are proteins that facilitate or accelerate specific chemical reactions allowing cells to function.

E.g. lipase, lactate and amylase.

19
Q

What are some examples or drugs that target enzymes?

A

. Ramapril - ACE inhibitor which relaxes arteriola smooth muscle.

. Simvastatin - HMG-CoA reductase that reducer production of cholesterol.

. Ibuprofen - Nonselective COX inhibitor decreasing production of prostaglandins which mediate pain, inflammation and fever, and thromboxane A2 which forms blood clots.

20
Q

What are some examples of non-specific function drugs?

A

. Osmotic laxatives (chemical changes) - Change environment around cell rather than in the cells itself, drawing water into GI tract.

. Barrier creams (physical changes) - Act as a barrier at the top layer of skin preventing water loss and irritant contact.

21
Q

What is meant by pharmacodynamic drug interactions?

A

They occur between drugs with additive or opposing effects. For example:

. Intentional additive effect - Combining antihypertensives
. Unintentional additive effect - Serotonin syndrome from combining tramadol with SSRIs
. Opposing effect - Reducing bronchodilation by a beta-2 antagonist prescribed with a non-selective beta-blocker.

22
Q

What are some groups vulnerable to pharmacodynamic interactions?

A

. Elderly
. Seriously ill patients
. Renal/hepatic issues
. Prescriptions from multiple sources
. Recreational drugs
. Herbal medicine