MindMap Gallery Pharmacology - Thyroid hormones and antithyroid drugs mind map
This is a mind map about pharmacology - thyroid hormones and antithyroid drugs, including an overview, pharmacological effects, clinical applications, adverse reactions, etc.
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036Thyroid hormones and antithyroid drugs
thyroid hormone
Thyroid: Largest endocrine gland Parathyroid hormone: regulates blood calcium and blood phosphorus Hyperthyroidism - afraid of heat, sweating a lot, prone to hunger and eating too much to lose weight; hypothyroidism - likes heat and hates cold, poor appetite
Overview
T4 → T3 under the action of peripheral tissue deiodinase
Thyroid hormones include tetraiodothyronine (thyroxine, T4, high content, slow and weak effects) and triiodothyronine (T3, low content, fast and strong effects) The pituitary gland secretes thyroid-stimulating hormone (TSH), which ① promotes thyroid synthesis and secretion ② promotes thyroid tissue hyperplasia
Pharmacological effects
Maintain normal growth and development - promote protein synthesis; promote the growth and development of bones and central nervous system
Cretinism, neonatal respiratory distress syndrome (T3T4 accelerates fetal lung development), myxedema
Promote metabolism and thermogenesis
Sugar: Promote glucose absorption and liver glycogen decomposition Lipids: Accelerate the oxidative decomposition of fats Protein: Large doses promote protein decomposition, small doses promote synthesis Increase oxygen consumption, increase basal metabolic rate, and increase heat production
Improve sympathetic-adrenal system reactivity - sympathetic nerve reactivity ↑, nervousness, irritability, tremor, increased heart rate, cardiac output ↑, blood pressure ↑
Clinical Application—Replacement Therapy for Hypothyroidism
Cretinism - early diagnosis and treatment, treatment of past, persistent mental retardation Myxedema - generally take tablets or powder, start with a small dose and gradually increase to a sufficient dose
Simple goiter - ①Those caused by iodine deficiency should supplement iodine; ②Insufficient endogenous hormones should be given an appropriate amount of thyroid hormone
other
① Patients with hyperthyroidism should also take T4 when taking antithyroid drugs ②Application of T4 after thyroid cancer surgery ③ Used for differential diagnosis of patients with high iodine uptake rate in T3 suppression test
Adverse reactions: Overdose - palpitations, hand tremors, sweating, weight loss, insomnia and other symptoms of hyperthyroidism, angina, heart failure, muscle tremors or spasms (stop the drug immediately and use beta-blockers to counteract it)
antithyroid drugs
The most common type of hyperthyroidism: toxic diffuse goiter (clinical manifestations - thyrotoxicosis, diffuse goiter, exophthalmos, pretibial myxedema) Surgical treatment, radiotherapy, drug treatment
Thioureas
Methiouracil, propylthiouracil; methimazole, carbimazole Excellent: Certain efficacy, safe, convenient and cheap Disadvantages: Slow onset of effect, long course of treatment
Pharmacological effects
Inhibits thyroid peroxidase, inhibits iodination and conjugation of tyrosine, and inhibits the synthesis of thyroid hormones
Inhibits the conversion of T4 into T3 in peripheral tissues (propylthiouracil quickly controls T3 levels and is the first choice for the treatment of severe hyperthyroidism and thyroid storm)
Attenuates β-receptor-mediated glucose metabolism
Immunosuppressive effect: Reduces thyroid-stimulating immune globulin, which also has a certain therapeutic effect on the cause of hyperthyroidism.
Methimazole: first choice in general situations Propylthiouracil: Thyroid storm, severe cases, early pregnancy
Clinical application
Medical treatment of hyperthyroidism - suitable for patients with mild symptoms and those who are not suitable for surgery or radioactive iodine therapy
Preparation before thyroid surgery (sulfur first, then iodine) Purpose: Control thyroid function and reduce post-operative complications and thyroid storm Disadvantages: TSH increases after using thioureas, causing gland hyperplasia and congestion. Treatment: Take a large amount of iodine two weeks before surgery
Treatment of thyroid storm: iodine first, then sulfur (large doses of iodine can inhibit the release of thyroid hormone)
Adverse reactions
gastrointestinal reactions
Anaphylaxis: most common Agranulocytosis: most severe, usually occurs 2-3 months after treatment
Goiter and hypothyroidism
Iodine and iodide
Pharmacological effects
Small dose: Iodine is a raw material for the synthesis of thyroid hormone, preventing simple goiter
High dose: antithyroid effect
①Inhibit thyroid proteolytic enzyme and inhibit thyroid hormone release ② Inhibit thyroid peroxidase and inhibit thyroid hormone synthesis ③Antagonize the effect of TSH
The effect is time-limited, and iodide cannot be used alone in the medical treatment of hyperthyroidism: large doses have a rapid and strong effect, taking effect in 1-2 days and reaching the maximum effect in 10-15 days. The concentration of iodine ions in the acinar cells increases to a certain concentration. The ability of cells to take up iodine automatically↓, the intracellular iodide ion concentration↓, and loses the effect of inhibiting hormone synthesis.
Clinical application
Small dose - prevention of simple goiter Large dose: ① Preoperative preparation for hyperthyroidism (sulfur first, then iodine, iodine solution is given 2 weeks before surgery to inhibit TSH's role in promoting gland hyperplasia, shrink and toughen the glands, reduce blood vessels, facilitate surgery and reduce bleeding) ②Treatment of thyroid storm (iodine first, then sulfur)
Adverse reactions
General reactions: Throat discomfort, metallic taste in the mouth, respiratory tract irritation, sinusitis, conjunctivitis, increased salivation, salivary gland enlargement Allergic reactions: fever, rash, dermatitis, angioedema, laryngeal edema, asphyxia Induce thyroid dysfunction: Long-term overdose induces hyperthyroidism, which can pass through the placenta and breast milk and cause thyroid dysfunction in newborns and infants.
beta-adrenoceptor blocking drugs
propranolol, metoprolol, atenolol
Pharmacological effects
Block beta receptors and improve symptoms of sympathetic-adrenergic system excitement caused by hyperthyroidism
Blocks cardiac β1 receptors, heart rate ↓; blocks central β receptors, reduces anxiety; blocks peripheral NA nerve terminal presynaptic membrane β2 receptors, ↓NA release
Proper ↓Thyroid hormone secretion
Clinical application - adjuvant medicine for hyperthyroidism and thyroid storm
radioactive iodine
Radioactive iodine is ¹³¹I, of which beta rays account for 99%, have a short range, destroy the thyroid parenchyma, and can be used to surgically remove part of the thyroid gland; gamma rays account for 1%, have a long range, and are used to measure the iodine uptake function of the thyroid gland
Clinical application
Treatment of hyperthyroidism - suitable for patients with hyperthyroidism who are not suitable for surgery, have relapsed after surgery, are ineffective with thioureas, or are allergic. Determine the iodine uptake function of the thyroid gland - hyperthyroidism (high iodine uptake rate, peak iodine uptake time shifts forward), hypothyroidism (low iodine uptake rate, peak iodine uptake time shifts later)
Advantages: safe, simple, effective, cheap Disadvantages: Slow action, difficult to control dosage, 2nd or 3rd treatment required (half a year apart)