PHARMACO OVERALL OBA QUESTION
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Questions and Answers

What is the primary mechanism of action of methotrexate in inhibiting cancer cell growth?

  • Inhibition of thymidylate synthase, leading to inhibition of DNA synthesis and repair (correct)
  • Inhibition of pyrimidine synthesis, leading to inhibition of protein synthesis
  • Inhibition of DNA polymerase, leading to inhibition of DNA replication
  • Inhibition of dihydrofolate reductase, leading to inhibition of purine synthesis

    • Which of the following cancers is NOT typically treated with low-dose methotrexate?

  • Rheumatoid arthritis
  • Breast cancer
  • Acute nonlymphocytic leukemia (correct)
  • Severe psoriasis

    • What is the primary use of 5-fluorouracil?

  • Treatment of acute nonlymphocytic leukemia
  • Treatment of superficial basal cell carcinomas
  • Treatment of slowly growing solid tumors (correct)
  • Treatment of inflammatory diseases

    • Which of the following is a common side effect of methotrexate?

    <p>Myelosuppression</p> Signup and view all the answers

    What is the mechanism of action of cytarabine?

    <p>Inhibition of DNA polymerase</p> Signup and view all the answers

    Which of the following is a use of 5-fluorouracil?

    <p>Treatment of superficial basal cell carcinomas</p> Signup and view all the answers

    What is the primary mechanism of action of centrally acting drugs in the management of hypertension?

    <p>Decreased sympathetic outflow from the vasomotor center in the brain</p> Signup and view all the answers

    Which of the following is a common side effect of clonidine?

    <p>Sedation</p> Signup and view all the answers

    What is a major concern when using clonidine in patients with renal disease?

    <p>Worsening of renal function</p> Signup and view all the answers

    Which of the following is an indication for the use of hydralazine in hypertension?

    <p>Moderate to severe hypertension</p> Signup and view all the answers

    What is a common side effect of hydralazine?

    <p>Reflex tachycardia</p> Signup and view all the answers

    Which of the following is a contraindication for the use of α-methyldopa?

    <p>Renal insufficiency</p> Signup and view all the answers

    What is the primary mechanism of action of α-methyldopa in the management of hypertension?

    <p>Inhibition of renin release and sodium retention</p> Signup and view all the answers

    Which of the following medications is often used to control pregnancy-induced hypertension and eclampsia?

    <p>α-Methyldopa</p> Signup and view all the answers

    What is the result of absorption of the recommended medication in the absence of food?

    <p>Improved absorption</p> Signup and view all the answers

    Which site on the mRNA-ribosome complex does the recommended medication block?

    <p>A site</p> Signup and view all the answers

    What is the effect of the recommended medication on bone growth in children?

    <p>Retardation of bone growth</p> Signup and view all the answers

    What is a common side effect of the recommended medication in pregnant and nursing mothers?

    <p>Yellow discoloration of teeth</p> Signup and view all the answers

    What is the mode of administration of macrolides?

    <p>Oral or parenteral</p> Signup and view all the answers

    What is the effect of macrolides on protein synthesis?

    <p>Inhibition of protein synthesis</p> Signup and view all the answers

    What is a common side effect of the recommended medication?

    <p>All of the above</p> Signup and view all the answers

    What is the effect of macrolides on the P450 enzyme?

    <p>Inhibition of P450 enzyme</p> Signup and view all the answers

    What is a contraindication for the recommended medication?

    <p>All of the above</p> Signup and view all the answers

    What is the recommended medication used to treat?

    <p>Superficial ocular infections</p> Signup and view all the answers

    What is the primary function of Progestin-only Pill (Mini Pill) in contraception?

    <p>To prevent ovulation and implantation</p> Signup and view all the answers

    Which of the following is NOT a side effect of Progestin-only Pill (Mini Pill)?

    <p>Aplastic anemia</p> Signup and view all the answers

    What is the mechanism of action of Iodide Salts in treating thyroid storm?

    <p>Block thyroid hormone release via negative feedback mechanism</p> Signup and view all the answers

    Which of the following is an advantage of Biguanides in treating type 2 diabetes?

    <p>Decrease in free fatty acid levels</p> Signup and view all the answers

    What is the primary mechanism of action of Sulfonylureas in treating type 2 diabetes?

    <p>Stimulate β-cells to secrete insulin</p> Signup and view all the answers

    Which of the following is a side effect of Glitazones?

    <p>Fluid retention</p> Signup and view all the answers

    What is the mechanism of action of Acarbose in treating type 2 diabetes?

    <p>Inhibit α-glucosidase enzyme in the intestine</p> Signup and view all the answers

    Which of the following is an indication for the use of Folic Acid Analog (Methotrexate)?

    <p>Acute lymphocytic leukemia in children</p> Signup and view all the answers

    What is the mechanism of action of Radioactive Iodine (RAI) therapy in treating hyperthyroidism?

    <p>Destroy abnormal thyroid cells by emitting radiation</p> Signup and view all the answers

    Which of the following is a contraindication for the use of Progestin-only Pill (Mini Pill)?

    <p>All of the above</p> Signup and view all the answers

    What is the primary mode of excretion for S. aureus infections?

    <p>Kidney</p> Signup and view all the answers

    What is the first-line treatment for Klebsiella infections?

    <p>Cephalosporins</p> Signup and view all the answers

    How do glycopeptides like Vancomycin inhibit bacterial cell wall synthesis?

    <p>By binding to the amino acid side chain of NAM molecules</p> Signup and view all the answers

    What is a common side effect of aminoglycosides like Gentamicin?

    <p>Ototoxicity</p> Signup and view all the answers

    How are aminoglycosides typically administered?

    <p>Intramuscularly or intravenously</p> Signup and view all the answers

    What is the mechanism of action of aminoglycosides in inhibiting protein synthesis?

    <p>Inhibiting the 30S ribosomal subunit</p> Signup and view all the answers

    Why should aminoglycosides be avoided in combination with other ototoxic drugs?

    <p>Because they can increase the risk of ototoxicity</p> Signup and view all the answers

    What is the consequence of irreversible binding of aminoglycosides to the 30S ribosomal subunit?

    <p>Irreversible damage to the 8th cranial auditory nerve</p> Signup and view all the answers

    Study Notes

    Antihypertensive Drugs

    • Clonidine:
      • Acts centrally to decrease sympathetic outflow from the vasomotor center in the brain, leading to decreased heart rate and blood pressure.
      • Indications: Hypertension complicated by renal disease, pregnant patients, and asthma.
      • Side effects: Sedation, depression, rebound hypertension, and crisis.
    • α-Methyldopa:
      • Acts centrally to decrease sympathetic outflow from the vasomotor center in the brain, leading to decreased heart rate and blood pressure.
      • Indications: Hypertension complicated by renal disease, pregnant patients, and asthma.
      • Side effects: Sedation, depression, rebound hypertension, and crisis.
    • Vasodilators:
      • Hydralazine:
        • Direct vasodilation of arteries and arterioles, leading to decreased peripheral resistance and blood pressure.
        • Indications: Moderate to severe hypertension, often combined with β blockers and diuretics.
        • Side effects: Reflex tachycardia, edema, headache, and nausea.

    Contraceptives

    • Combined Oral Contraceptives (COCs):
      • Contain estrogen and progestin.
      • Mechanism of action: Inhibit ovulation, thicken cervical mucus, and alter the lining of the uterus.
      • Side effects: Nausea, vomiting, headache, breast tenderness, weight gain, and chloasma.
      • Contraindications: Women with a history of thrombophlebitis, stroke, or myocardial infarction.
    • Progestin-only Pill (Mini Pill):
      • Contains progestin only.
      • Mechanism of action: Thickens cervical mucus, alters the lining of the uterus, and inhibits ovulation.
      • Side effects: Irregular menstrual cycles, breast tenderness, and weight gain.
      • Contraindications: Women with a history of thrombophlebitis, stroke, or myocardial infarction.
    • Emergency Hormonal Contraception:
      • Contains high-dose progestin only.
      • Mechanism of action: Delays ovulation and prevents implantation.
      • Side effects: Nausea, vomiting, headache, and breast tenderness.
      • Contraindications: Women with a history of thrombophlebitis, stroke, or myocardial infarction.

    Hormone Replacement Therapy

    • Levothyroxine (Synthetic T4):
      • Indications: Hypothyroidism.
      • Mechanism of action: Replaces thyroid hormone.
      • Side effects: None.
    • Liothyronine (Synthetic T3):
      • Indications: Acute emergency in myxedema coma.
      • Mechanism of action: Replaces thyroid hormone.
      • Side effects: None.

    Antithyroid Drugs

    • Thionamides:
      • Propylthiouracil (PTU):
        • Indications: Hyperthyroidism.
        • Mechanism of action: Inhibits hormone synthesis through irreversible binding to thyroid peroxidase.
        • Side effects: Agranulocytosis, thrombocytopenia, and SLE-like syndrome.
      • Methimazole (MMI):
        • Indications: Hyperthyroidism.
        • Mechanism of action: Inhibits hormone synthesis through irreversible binding to thyroid peroxidase.
        • Side effects: Agranulocytosis, thrombocytopenia, and SLE-like syndrome.
    • Ionic Inhibitors:
      • Perchlorate (CIO4-):
        • Indications: Hyperthyroidism.
        • Mechanism of action: Inhibits the uptake of iodine into the thyroid gland.
        • Side effects: Aplastic anemia and gastric ulcer.
    • Radioactive Iodine (RAI) Therapy:
      • I131:
        • Indications: Graves' disease and multinodular toxic goiter.
        • Mechanism of action: Selectively taken up by the abnormal thyroid gland, emitting both χ-rays and β radiation, and destroying thyroid cells.
        • Side effects: None.
    • Iodide Salts:
      • KI, SSKI, and Iodoral:
        • Indications: Emergency management of thyroid storm, presurgery for subtotal thyroidectomy, and heavy menstrual bleeding.
        • Mechanism of action: Blocks thyroid hormone release and decreases the size and vascularity of the thyroid gland.
        • Side effects: Iodism and skin rashes.

    Antidiabetic Drugs

    • Sulfonylureas:
      • Tolbutamide and Glipizide:
        • Mechanism of action: Binding to SUR1 on KAPT channels, closing the channel, and increasing calcium influx, leading to insulin release.
        • Side effects: Hypoglycemia, weight gain, and allergies.
    • Biguanides:
      • Metformin:
        • Mechanism of action: Inhibiting gluconeogenesis, decreasing free fatty acid, LDL, and triglycerides, and increasing insulin sensitivity.
        • Side effects: Hepatotoxicity, GI disturbance, and lactic acidosis.
    • Glitazones:
      • Troglitazone and Rosiglitazone:
        • Mechanism of action: Activating PPARɣ, increasing insulin sensitivity, and improving β-cell function.
        • Side effects: Fluid retention, CHF, and hepatotoxicity.
    • Acarbose:
      • Mechanism of action: Competitive inhibitor of α-glucosidase, slowing down the digestion of carbohydrates and decreasing glucose absorption.
      • Side effects: Abdominal discomfort, bloating, flatulence, and diarrhea.

    Cancer Chemotherapy

    • Cell Cycle Specific Agents (CCS):
      • Folic Acid Analogues:
        • Methotrexate:
          • Mechanism of action: Inhibiting dihydrofolate reductase, blocking the synthesis of thymidylate and purines.
          • Side effects: Bone marrow suppression, nephrotoxicity, and myelosuppression.
      • Pyrimidine Analogues:
        • 5-Fluorouracil:
          • Mechanism of action: Inhibiting thymidylate synthesis.
          • Side effects: Myelosuppression and diarrhea.
      • Cytarabine:
        • Mechanism of action: Inhibiting DNA polymerase.
        • Side effects: Myelosuppression and urinary tract infections.

    Antibiotics

    • Glycopeptides:

      • Vancomycin:
        • Mechanism of action: Binding to the amino acid side chain of NAM molecules, interfering with peptidoglycan synthesis.
        • Side effects: Ototoxicity and nephrotoxicity.

    • Protein Synthesis Inhibitors:

      • Aminoglycosides:
        • Gentamicin:
          • Mechanism of action: Binding to the 30S subunit of ribosomal RNA, inhibiting protein synthesis.
          • Side effects: Ototoxicity and nephrotoxicity.### Tetracycline

    • Absorption of tetracycline is improved in the absence of food, but decreased in the presence of milk.

    • Tetracycline inhibits aminoacyl transferase, blocking the binding of tRNA to the acceptor site (A site) on the mRNA-ribosome complex, preventing the continuation of protein synthesis.

    • Side effects of tetracycline include:

      • Yellow discoloration of teeth in young children
      • Retardation of bone growth in children
      • Photosensitivity reactions (severe sunburn) in pregnant and nursing mothers
      • Superinfection (candidiasis, pseudomembranous colitis)
      • Nephrotoxicity (especially when combined with other nephrotoxic drugs and in renal disease)

    Macrolide

    • Used to treat superficial ocular infections involving conjunctiva and cornea
    • Can be administered orally or parenterally
    • Binds reversibly to the 50S subunit
    • Acts as a P450 inhibitor, which can affect the bioavailability of other drugs

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    Description

    This quiz covers the mechanisms of action and uses of various chemotherapy medications, including methotrexate, 5-fluorouracil, and cytarabine. It also explores the cancers that are typically treated with these medications and their common side effects.

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