ADME Flashcards

1
Q

Meningitis and BBB

A

meningitis is inflammation of membranes (meninges) surronding spinal cord , integrity of BBBcan be comprimised

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2
Q

How to treat meningitis

A

Antibiotics that do not pass BBB
E.g Benzylpenicillin

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3
Q

Give two antiemetics and explain if they cross BBB or not

A

Domperidone and Metocloperamide both inhibits dopamine (dopamine receptor antagonist)
Metocloperamide cross BBB
Doperidone do not cross BBB

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4
Q

What are the pharmacokinetic characteristics and clinical uses of Propofol?

A

Propofol is an IV general anesthetic following a 2-compartment model. It is highly lipid-soluble, used for rapid induction of anesthesia with an onset of action within 20 seconds and a short duration of 5-10 minutes. Its elimination half-life is 2-30 hours, and it requires careful dosing to maintain anesthesia without prolonged effects.

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5
Q

What are zero-order kinetics in drug metabolism?

A

Zero-order kinetics occur when the rate of drug elimination is constant and does not change with increasing drug concentration. This happens when the drug-metabolizing enzymes are saturated. Classic examples include phenytoin and ethanol. Unlike first-order kinetics where elimination is proportional to the drug concentration, in zero-order kinetics, a constant amount of drug is eliminated per unit time.

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6
Q

What are the potential teratogenic effects of Phenytoin when used during pregnancy?

A

Phenytoin use during pregnancy can be associated with craniofacial abnormalities, hypoplasia of distal phalanges, growth and mental deficiency, collectively known as fetal hydantoin syndrome.

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7
Q

What are the risks of using Valproate during pregnancy?

A

Valproate is associated with a high risk of neural tube defects and can lead to learning difficulties in the child; it is considered highly teratogenic.

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8
Q

How does Carbamazepine compare with Phenytoin in terms of teratogenic risk during pregnancy?

A

How does Carbamazepine compare with Phenytoin in terms of teratogenic risk during pregnancy?

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9
Q

Firstline for tonic clonic seizures

A

Lamotigrine

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10
Q

Prevents these drugs during pregnancy depression

A

SSRI citolopram and setaline
Associates cardiac septal defects

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11
Q

What are the pharmacological actions of St. John’s Wort?

A

St. John’s Wort has SSRI-like actions and can increase serotonin levels in the brain, which may help improve mood and relieve symptoms of depression.

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12
Q

What is a major risk when combining St. John’s Wort with SSRIs?

A

The combination can lead to Serotonin Syndrome, a potentially life-threatening condition due to excessive serotonin levels.

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13
Q

How does St. John’s Wort affect drug metabolism?

A

It is an enzyme inducer, which can accelerate the metabolism of certain drugs, reducing their effectiveness.

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14
Q

Which drugs can have their effectiveness reduced by St. John’s Wort?

A

St. John’s Wort can reduce the effectiveness of oral contraceptives, anti-HIV drugs, and immunosuppressants like Ciclosporin.

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15
Q

What is the therapeutic window for lithium treatment?

A

The therapeutic window for lithium is narrow, typically 0.4-1 mmol/L, requiring close monitoring to avoid toxicity.

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16
Q

What factors influence the plasma concentration of lithium?

A

Plasma concentration of lithium is determined by the kidney function, specifically eGFR, and electrolyte balance in the body.

17
Q

Why is therapeutic drug monitoring (TDM) important for lithium therapy?

A

TDM is crucial for lithium because of its narrow therapeutic window and the risk of toxicity; it ensures plasma levels stay within the safe and effective range of 0.4-1 mmol/L.

18
Q

Interactions with John wort increases SRRI

A

Oral contraceptives (Ethinylestradiol)
Anti HIV (Indinavir)
Immunosupressants ( Ciclosporin)
SSRI (Sertaline)