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What is the primary mechanism of action of methotrexate in inhibiting cancer cell growth?
Which of the following cancers is NOT typically treated with low-dose methotrexate?
What is the primary use of 5-fluorouracil?
Which of the following is a common side effect of methotrexate?
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What is the mechanism of action of cytarabine?
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Which of the following is a use of 5-fluorouracil?
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What is the primary mechanism of action of centrally acting drugs in the management of hypertension?
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Which of the following is a common side effect of clonidine?
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What is a major concern when using clonidine in patients with renal disease?
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Which of the following is an indication for the use of hydralazine in hypertension?
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What is a common side effect of hydralazine?
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Which of the following is a contraindication for the use of α-methyldopa?
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What is the primary mechanism of action of α-methyldopa in the management of hypertension?
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Which of the following medications is often used to control pregnancy-induced hypertension and eclampsia?
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What is the result of absorption of the recommended medication in the absence of food?
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Which site on the mRNA-ribosome complex does the recommended medication block?
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What is the effect of the recommended medication on bone growth in children?
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What is a common side effect of the recommended medication in pregnant and nursing mothers?
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What is the mode of administration of macrolides?
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What is the effect of macrolides on protein synthesis?
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What is a common side effect of the recommended medication?
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What is the effect of macrolides on the P450 enzyme?
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What is a contraindication for the recommended medication?
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What is the recommended medication used to treat?
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What is the primary function of Progestin-only Pill (Mini Pill) in contraception?
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Which of the following is NOT a side effect of Progestin-only Pill (Mini Pill)?
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What is the mechanism of action of Iodide Salts in treating thyroid storm?
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Which of the following is an advantage of Biguanides in treating type 2 diabetes?
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What is the primary mechanism of action of Sulfonylureas in treating type 2 diabetes?
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Which of the following is a side effect of Glitazones?
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What is the mechanism of action of Acarbose in treating type 2 diabetes?
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Which of the following is an indication for the use of Folic Acid Analog (Methotrexate)?
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What is the mechanism of action of Radioactive Iodine (RAI) therapy in treating hyperthyroidism?
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Which of the following is a contraindication for the use of Progestin-only Pill (Mini Pill)?
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What is the primary mode of excretion for S. aureus infections?
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What is the first-line treatment for Klebsiella infections?
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How do glycopeptides like Vancomycin inhibit bacterial cell wall synthesis?
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What is a common side effect of aminoglycosides like Gentamicin?
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How are aminoglycosides typically administered?
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What is the mechanism of action of aminoglycosides in inhibiting protein synthesis?
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Why should aminoglycosides be avoided in combination with other ototoxic drugs?
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What is the consequence of irreversible binding of aminoglycosides to the 30S ribosomal subunit?
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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.
- Hydralazine:
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.
- Propylthiouracil (PTU):
- 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.
- Perchlorate (CIO4-):
- 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.
- I131:
- 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.
- KI, SSKI, and Iodoral:
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.
- Tolbutamide and Glipizide:
- 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.
- Metformin:
- Glitazones:
- Troglitazone and Rosiglitazone:
- Mechanism of action: Activating PPARɣ, increasing insulin sensitivity, and improving β-cell function.
- Side effects: Fluid retention, CHF, and hepatotoxicity.
- Troglitazone and Rosiglitazone:
- 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.
- Methotrexate:
- Pyrimidine Analogues:
- 5-Fluorouracil:
- Mechanism of action: Inhibiting thymidylate synthesis.
- Side effects: Myelosuppression and diarrhea.
- 5-Fluorouracil:
- Cytarabine:
- Mechanism of action: Inhibiting DNA polymerase.
- Side effects: Myelosuppression and urinary tract infections.
- Folic Acid Analogues:
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.
- Vancomycin:
-
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
- Gentamicin:
- Aminoglycosides:
-
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.
