Methotrexate Mechanism and Indications

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What is the primary mechanism of action of this medication?

Inhibition of purine and pyrimidine synthesis

What is a common indication for this medication?

Treatment of leukemia

What is the primary route of excretion for this medication?

Urine

What is a common adverse effect of this medication?

Nausea and vomiting

What is a contraindication for this medication?

Pregnancy

What laboratory test should be monitored regularly in patients taking this medication?

Complete Blood Count (CBC)

Study Notes

Mechanism of Action

  • Inhibits dihydrofolate reductase, an enzyme involved in the synthesis of purines and pyrimidines
  • Decreases the production of nucleotides, thereby inhibiting cell division and growth

Indications

  • Cancer treatment (e.g., leukemia, lymphoma, breast cancer)
  • Autoimmune diseases (e.g., rheumatoid arthritis, psoriasis)
  • Ectopic pregnancy
  • Abortion (in combination with misoprostol)

Pharmacokinetics

  • Oral bioavailability: 33-75%
  • Peak plasma concentration: 1-2 hours
  • Half-life: 3-10 hours
  • Excreted mainly in the urine

Adverse Effects

  • Gastrointestinal: nausea, vomiting, diarrhea, stomatitis
  • Hematological: bone marrow suppression, anemia, thrombocytopenia
  • Hepatic: elevated liver enzymes
  • Dermatological: skin rash, alopecia
  • Pulmonary: pneumonitis

Contraindications

  • Pregnancy (category X)
  • Breastfeeding
  • Severe renal impairment
  • Severe hepatic impairment
  • Active infection

Monitoring

  • Complete Blood Count (CBC) regularly
  • Liver function tests (LFTs) regularly
  • Renal function tests regularly
  • Monitor for signs of infection and bleeding

Mechanism of Action

  • Inhibits dihydrofolate reductase, an enzyme involved in purine and pyrimidine synthesis
  • Decreases nucleotide production, inhibiting cell division and growth

Indications

  • Cancer treatment (e.g., leukemia, lymphoma, breast cancer)
  • Autoimmune diseases (e.g., rheumatoid arthritis, psoriasis)
  • Ectopic pregnancy
  • Abortion (in combination with misoprostol)

Pharmacokinetics

  • Oral bioavailability: 33-75%
  • Peak plasma concentration: 1-2 hours
  • Half-life: 3-10 hours
  • Mainly excreted in the urine

Adverse Effects

  • Gastrointestinal: nausea, vomiting, diarrhea, stomatitis
  • Hematological: bone marrow suppression, anemia, thrombocytopenia
  • Hepatic: elevated liver enzymes
  • Dermatological: skin rash, alopecia
  • Pulmonary: pneumonitis

Contraindications

  • Pregnancy (category X)
  • Breastfeeding
  • Severe renal impairment
  • Severe hepatic impairment
  • Active infection

Monitoring

  • Regular Complete Blood Count (CBC)
  • Regular liver function tests (LFTs)
  • Regular renal function tests
  • Monitoring for signs of infection and bleeding

Learn about the mechanism of action of methotrexate, its indications, and pharmacokinetics. This quiz covers its use in cancer treatment, autoimmune diseases, and more.

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