Transporters as drug targets Flashcards

1
Q

Name the 3 major types of transmembrane Transporter proteins.

A

1) Passive transport - channels and transporter proteins facilitate movement DOWN conc gradient
2) Active - Energy is used from ATP to pump solutes UP the conc gradient
3) Coupled (Symporters and Antiporters) - use potential energy to move solutes up their gradient

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2
Q

Transporters in the kidney are known as Diuretics. TRUE or FALSE ?

A

TRUE

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3
Q

What is the role of diuretics and how do thy carry out this role?

A

Increase urine output;

by inhibiting the sodium pumps therefore inhibiting water being reabsorbed

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4
Q

Na+K+ATPase is the driving force behind the re absorption of Na+ (throughout the nephron). TRUE or FALSE ?

A

TRUE

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5
Q

Digoxin acts on Na+K+ATPase and does what ?

A

Increases the power of each cardiac muscle contraction therefore increases cardiac output

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6
Q

What happens during excitation of Cardiac tissue ?

A

Influx of Calcium and release of calcium from Intracellular stores

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7
Q

Calcium promotes myofibre contraction. TRUE or FALSE ?

A

TRUE

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8
Q

Digoxin inhibits Na+K+ Antiporter. TRUE or FALSE ?

A

TRUE

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9
Q

Heart failure is as a result of inadequate cardiac output. TRUE or FALSE ?

A

TRUE

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10
Q

Antidepressants act as transporters in the brain. TRUE or FALSE ?

A

TRUE

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11
Q

Name 4 examples of Antidepressants

A

1) SSRRI’s (serotonin specific reuptake inhibitors)
2) SNRI’s (serotonin and nor-ad reuptake inhibitors)

3) Nor-ad
4) Dopamine

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12
Q

What do Tri-cyclic antidepressants do ?

A

Inhibits 1) serotonin and nor-ad reuptake

2) Other off target effects.

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13
Q

Proton pump inhibitors regulate stomach acidity. TRUE or FALSE ?

A

TRUE

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14
Q

How do proton pump inhibitors work ? Give an example of a drug that acts as a proton pump inhibitor.

A

1) bind irreversibly to proton pumps
2) Inhibit proton excretion to the stomach
3) facilitates healing of gastric ulcers

-Omeprazole

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15
Q

Proton pump acts on H+K+ATPase. TRUE or FALSE ?

A

TRUE

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16
Q

What is the role of Ezetimibe ?

A

Reduces elevated cholesterol levels;

by inhibiting absorption of cholesterol across the internal brush border

17
Q

Transporters can facilitate or inhibit drug action. TRUE or FALSE ?

A

TRUE

18
Q

How do facilitating drug transporters work and name an example of a drug that acts in this way?

A

by acting as drug pumps therefore assisting the drug in reaching its target.
e.g: Organic anion transporter

19
Q

How do inhibiting drug transporters work and name an example of a drug that acts in this way?

A

by acting as dug efflux pumps; therefore prevent drug from reaching its target
e.g: PgP