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2a- Pharmacology > Drugs - enzymes and transporters > Flashcards

Drugs - enzymes and transporters Flashcards

1
Q

What is an enzyme inhibitor?

A

a molecule that binds to anenzymeand (normally) decreases itsactivity

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2
Q

How does an enzyme inhibitor work?

A

An enzyme inhibitor prevents the substratefrom entering the enzyme’sactive site and prevents it fromcatalyzingits reaction

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3
Q

What are the 2 types of enzyme inhibitors?

A

Irreversible
Reversible

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4
Q

How do irreversible inhibitors work?

A

usually react with the enzyme and change it chemically (e.g. viacovalent bondformation)

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5
Q

How do reversible inhibitors work?

A

bindnon-covalentlyand different types of inhibition are produced depending on whether these inhibitors bind to theenzyme, the enzyme-substrate complex, or both

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6
Q

What does inhibiting ACE do?

A

Decreases RAAS system, reduces angiotensin II, so less Na+ and water retained, lowers BP

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7
Q

What does inhibiting HMG-CoA reductase do?

A

Rate limiting step, reduced cholesterol production

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8
Q

What are the passive ways of transporting drugs and ions?

A

Symporter
Channels

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9
Q

What ions travel by symporters?

A

Na/K/2Cl
NaCl

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10
Q

What ions travel by channels?

A

Na
Ca
K
Cl

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11
Q

What is the active way of transporting drugs and ions?

A

ATP-ases

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12
Q

What ions travel through ATP-ases?

A

Na/K
K/H

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13
Q

What are the 3 main protein ports?

A

Uniporters
Symporters
Antiporters

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14
Q

What do uniporters do?

A

Use energy from ATP to pull molecules in

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15
Q

What do symporters do?

A

use the movement in of one molecule to pull in another molecule against a concentration gradient

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16
Q

What do antiporters do?

A

one substance moves against its gradient, using energy from the second substance (mostly Na+, K+ or H+) moving down its gradient

17
Q

What’s an example of a symporter?

A

NKCC (Na K Cl co transporter)

18
Q

What does furosemide do?

A

Inhibits luminal NKCC symporter in LOH causing Na, K, Cl to be lost in urine

19
Q

What are examples of ion channels?

A
  • Epithelial (Sodium): heart failure
  • Voltage-gated (Calcium, Sodium): nerve, arrhythmia
  • Metabolic (Potassium): diabetes
  • Receptor Activated (Chloride): epilepsy
20
Q

What’s are examples of ATP-ases?

A

Sodium pump (Na/K ATP-ase)
Proton pump (K/H ATP-ase)

21
Q

What is digitoxin?

A
  1. inhibits the Na+/K+ ATPase, mainly in the myocardium
  2. This inhibition causes an increase in intracellular Na, resulting in decreased activity of the Na-Ca exchanger and increases intracellular Ca
  3. This lengthens the cardiac action potential, which leads to a decrease in heart rate
22
Q

What is digitoxin used for?

A

atrial fibrillation, atrial flutter, and heart failure

23
Q

What does omeprazole do?

A

Is an irreversible inhibitor of H/K ATP-ase
Is a PPI (proton pump inhibitor)

24
Q

What are organophosphates?

A

Irreversible inhibitors of cholinesterase

25
Q

What are some examples of organophosphates?

A
  • Insecticides (Diazinon)
  • Nerve gases (Sarin)
26
Q

What are the muscarinic and nicotinic effects of organophosphates?

A
  • Muscarinic – salivation, defaecation, urination, bradycardia, hypotension
  • Nicotinic – twitching, severe weakness paralysis, diaphragm
27
Q

What are the effects on the CNS from organophosphates?

A

confusion, loss of reflexes, convulsions, coma

28
Q

What is simvastatin?

A

A statin (enzyme)

29
Q

What is ramipril?

A

ACE inhibitor (enzyme)

30
Q

What is aspirin?

A

COX inhibitor (IRREVERSIBLE enzyme inhibitor)

31
Q

What is paracetamol?

A

COX inhibitor (enzyme)

32
Q

What determines the duration and intensity of a drug?

A

Rate of metabolism

33
Q

What are the major enzymes involved in drug metabolism?

A

CYPs (eg. CYP450) involved in 75% drug metabolism

34
Q

What are ENaCs (epithelial Na channels)?

A

Causes reabsorption of Na+ ions at the collecting ducts of the kidney’s nephrons (also in colon, lung and sweat glands)

35
Q

What drug targets ENaCs?

A

Amiloride
Thiazide
Work as anti-hypertensive

36
Q

Where are VDCCs (voltage gated Calcium channels) found?

A

found in the membrane of excitable cells (e.g. muscle, glial cells, neurons, etc.)
At physiologic or resting membrane potential, VDCCs are normally closed

37
Q

What drug targets VDCCs?

A

Amlodipine
- Causes vasodilation and a reduction peripheral vascular resistance, lowering blood pressure
- Also prevents excessive constriction in the coronary arteries

38
Q

How do receptor-mediated (chloride) channels work?

A

Ligand-gated ion channels (ionotropic receptors), open to allow ions to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand) such as a neurotransmitter
an example of receptor is GABA -A Receptor

39
Q

What drug works on receptor-mediated (chloride) receptors?

A

Barbiturates increase the permeability of the channel to chloride on GABA A receptors

2a- Pharmacology (10 decks)

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