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PMP 201 Patient-Centred Learning > Pharmacokinetics & drug interactions of antihypertensives > Flashcards

Pharmacokinetics & drug interactions of antihypertensives Flashcards

1
Q

Pharmacokinetics

A
  • Accumulation
  • Absorption
  • Distribution
  • Metabolism
  • Excretion
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2
Q

How can ADME be effected

A
  • Rate and extent to which drugs are absorbed
  • Rate and path of elimination from the body
  • Relationship between drug and plasma
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3
Q

Absorption

A
  • Route of administration significantly affected
  • Oral most common
  • pH effects drug solubility
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4
Q

Distribution

A
  • Anti-hypertensive drugs often target specific sites such as blood vessels and kidney
  • Proteins binding effect distribution slower
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5
Q

Metabolism

A
  • Most are metabolized in liver by haptic enzymes
  • Cytochrome P450 mostly metabolize
  • Broken down result in formation of active and inactive metabolites
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6
Q

Elimination

A

Rate of drug elimination is due to GFR rate and other factors

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7
Q

Additive interaction

A
  • Addition of two drugs which causes and equal effect to sum of individual effect
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8
Q

Synergistic interaction

A
  • Combination of drugs cause greater effect - control BP
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9
Q

Antagonistic interaction

A
  • Interaction of two drugs cancels out the individual effects
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10
Q

ACEi (Ramipril)

A
  • Producing prodrugs which inhibits ACE
  • Low angiotensin II and RAAS activity
  • Decrease blood flow and decrease blood volume
  • decrease sympathetic activity
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11
Q

Side effects of Ramipril

A
  • Hypotension
  • Hypokalemia
  • Dry cough
  • Bad taste
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12
Q

ACE inhibitor food interaction

A
  • High sodium and potassium meals counteracts effects of ACE inhibitors
  • Increase BP and interfere with balance of electrolytes
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13
Q

Drug to Drug interaction with ACEi

A
  • Concurrent use of ACEi and non-steroidal anti-inflammatory drugs reduce effectiveness of ACE
  • Increase risk of renal impairment by contacting vasodilatory effects
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14
Q

Drug and herbal interaction with ACEi

A
  • St John warts with ACEi induce the distribution metabolism and excretion so ACEi breaks down faster
  • Doesn’t reach therapeutic effect
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15
Q

CYP450 inducers

A
  • Concurrent use of rifampin antibiotic is a potent CYP450 inducer
  • Accelerate breakdown of ACEi reducing the effectiveness not reaching therapeutic effect
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16
Q

CYP450 inhibitors

A
  • Fluoxetine which a serotonin reuptake inhibitor and CYP450 repressor inhibit metabolism
  • Increase levels in blood therefore more side effects
17
Q

Losartan

A
  • Blocking the AT1 receptor
  • Opens up the arteries lowering BP and increasing blood to heart
  • Metabolized by CYP450
18
Q

Losartan drug to drug interaction

A
  • Co-administer ARB with Ketoconazole cause further decrease in BP which leads to fainting
19
Q

Losartan and food interaction

A
  • Grapefruit inhibit metabolism of ARB
  • Increase drug level in blood
  • prolong low BP with side effects
20
Q

Drug herbal interaction losartan

A
  • St john warts acts as a drug inducer of CYP3A4 increase metabolism of ARB
  • Unable to control BP reduced effectiveness
21
Q

CYP450 inducer with Losartan

A
  • Rifampin is potent inducer of CYP3A4
  • Lowers plasma concentration requires higher dosage
22
Q

CYP450 inhibitor

A
  • Co-administer with CYP2C9 fluconazole involved in metabolism and repressing cytochrome P450
  • Enhance therapeutic effect
23
Q

Pharmacokinetic drug interaction when taking losartan

A
  • Hypokalemia
  • Hypotension
  • Renal impairment
24
Q

Calcium channel adverse effect

A
  • Bradycardia
  • Abnormal pain and nausea
  • Dizzy drowsy and flushing
25
Q

Calcium channel interaction with statin

A
  • Increase serum levels of the statins causing statin toxicity and muscle pain
26
Q

Calcium channel and grapefruit interaction

A
  • Acts as a CYP450 inhibitor with an increase of CCB in blood cause increase side effect
27
Q

Hawthorn and Calcium channel blocker interaction

A
  • Cause Additive effects as it is a mild vasodilator enhance antihypertensive effects
28
Q

Indapamide

A
  • Inhibit NA+/Cl- co-transporter reducing sodium reabsorption
  • Decrease peripheral resistance
  • Decrease systolic BP
29
Q

Adverse effects of indapamide

A
  • Postural hypotension
  • Hypoglycemia
  • Hypokalemia
  • Cardiac arrythmias
  • Electrolyte imbalance
30
Q

Drug interaction indapamide

A

ACE and ARB cause very rapid fall in blood pressure

31
Q

Alpha-blockers and indapamide

A
  • Hypotensive effect during first dose
32
Q

Indapamide interaction with NSAID

A
  • Combination of NSAID with diuretics
  • Inhibits renal blood flow and decreases the efficacy of thiazides
33
Q

Licorice with indapamide

A
  • Decreased potassium levels and increased BP
  • Inhibition of cortisol breakdown cause water retention
34
Q

Carbamazepine and CYP450 inducer

A
  • Antiepileptic with CYP450 inducer increase metabolism of thiazide reducing blood levels
35
Q

Amiodarone and CYP450 repressor

A
  • Inhibit metabolism of thiazides increase blood levels diuretic and antihypertensive
36
Q

Inhibitors of CYP450
SICKFACE.COM acronym

A
  • Sodium valproate
  • Isoniazid
  • Cimetidine
  • Ketoconazole
  • Fluconazole
  • Amiodarone
  • Chloramphenicol
  • Erythromycin
  • Ciprofloxacin
  • Omeprazole
  • Metronidazole
    (increase BP)
37
Q

Inducers of CYP450
BS CRAP GPS

A
  • Barbiturates
  • St johns wart
  • Carbamazepine
  • Rifampin
  • Alcohol (Chronic)
  • Phenytoin
  • Griseofulvin
  • Phenobarbital
  • Sulfonylureas

(Decrease BP)

PMP 201 Patient-Centred Learning (51 decks)

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