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MindMap Gallery 6. Drugs that act on the endocrine system
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6. Drugs that act on the endocrine system
This is a mind map about six drugs that act on the endocrine system, including insulin and oral hypoglycemic drugs, sex hormone drugs and contraceptives, thyroid hormones and antithyroid drugs, etc.
Edited at 2024-03-09 11:23:53
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6. Drugs that act on the endocrine system
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- Outline
Drugs that act on the endocrine system
antihistamines
H1 receptor antagonist
Representative medicine
generation
Diphenhydramine
promethazine
Chlorpheniramine
Cyproheptadine
second generation
astemizole
Terfenadine
Cetirizine
Loratadine
Pharmacological effects
H1 receptor blocking effect
central role
The second generation is difficult to pass through the blood-brain barrier, so the central effect is weak or has almost no central sedative and anticholinergic effects.
anticholinergic effects
Has weak α-receptor antagonism and local anesthetic effects
Clinical application
allergic disease
motion sickness and vomiting
Quiet hypnosis
Adverse reactions
Central depressant effects, most common with diphenhydramine and promethazine
gastrointestinal reactions
Occasionally granulocytopenia, thrombocytopenia, hemolytic anemia, etc.
Astemizole and terfenadine can cause serious arrhythmias and should be noted
Not suitable for patients with glaucoma
mast cell stabilizer
Also known as allergic response mediator blockers
Representative drugs are sodium cromoglycate, ketotifen, and olopatadine
leukotriene receptor antagonist
Montelukast, Prolukast, Ibudilast
Thromboxane A2 receptor antagonist
Situlast
Other allergy medicines
Tranilast
calcium supplement
Calcium Gluconate and Calcium Chloride
Calcium can reduce or relieve allergic symptoms. It is usually injected intravenously and takes effect quickly.
Glucocorticoids
Currently, when used for allergic diseases, topical administration methods are mostly used, including inhalants, nasal agents, ophthalmic agents and external dermal dosage forms.
H2 receptor antagonist
Specifically blocks gastric parietal cell H2 receptors and antagonizes gastric acid secretion caused by histamine or histamine receptor agonists.
Representative medicine
Cimetidine
Ranitidine
Famotidine
nizatidine
Rosatidine
Mainly used for the treatment of gastric and duodenal ulcers
Drugs that affect autologous bioactive substances
Sex hormones and contraceptive pills
sex hormone drugs
Estrogens and anti-estrogens
Estrogens
Estradiol
Clinically, intramuscular injection or topical administration is used
Pharmacological effects
Promote female sexual maturity
For underage females, it can promote the development and maturity of female secondary sexual characteristics and sexual organs.
For adult women, it can maintain female secondary sexual characteristics, promote ovulation with the assistance of progesterone, transform the endometrium into the secretory phase, and form a menstrual cycle; improve the sensitivity of uterine smooth muscle to oxytocin
Estrogen stimulates the proliferation of vaginal epithelium and causes keratinization of superficial cells
Regulate endocrine effects
It can act on the feedback function of the hypothalamus and pituitary system to inhibit the secretion of gonadotropin-releasing hormone, thus inhibiting ovulation.
Inhibits the stimulating effect of prolactin on the mammary gland, reducing milk secretion
Antiandrogens
Effects on metabolism
There is mild water and sodium retention, causing elevated blood pressure
Increase bone calcium salt deposition, accelerate epiphyseal closure, promote puberty growth and development, and prevent osteoporosis in women
Clinical application
menopausal syndrome
Ovarian insufficiency and amenorrhea
functional uterine bleeding
Breast swelling and pain and breast withdrawal
Prostate cancer and adolescent acne
Adverse reactions
If you have a lack of appetite, nausea, vomiting, dizziness, etc., you should start with a small amount and increase the amount gradually to reduce the reaction.
Prolonged use may cause bleeding due to excessive endometrial hyperplasia, so patients with endometritis should use with caution.
Large amounts of estrogen can cause edema, hypertension, and aggravate heart failure. Cholestatic jaundice can occasionally be seen, so patients with poor liver function should use with caution.
Antiestrogens
clomiphene
Moderate anti-estrogenic effect, weak estrogenic activity
Can promote the secretion of gonadotropins and induce ovulation
For the treatment of functional infertility, amenorrhea and menstrual disorders caused by long-term use of contraceptive pills
Long-term use of large doses can cause ovarian hypertrophy and is contraindicated in patients with ovarian cysts.
progestins
progesterone
Pharmacological effects
On the basis of the effect of estrogen, progesterone can promote the continued thickening, congestion, and glandular proliferation of the endometrium, changing it from the proliferative phase to the secretory phase, which is beneficial to the implantation of the pregnant egg and embryo development.
Reduce the sensitivity of the uterus to oxytocin, inhibit uterine contraction, and have a miscarriage effect
Works with estrogen to promote the development of mammary gland alveoli and prepare for lactation
Large doses can feedbackly inhibit the secretion of luteinizing hormone from the anterior pituitary gland, thereby inhibiting ovulation.
Clinical application
functional uterine bleeding
Dysmenorrhea and endometriosis
Threatened abortion and habitual abortion
For threatened abortions with insufficient luteal corpus function, progesterone 10-20 mg can be injected every other day or every day. The medication can be discontinued 7 days after vaginal bleeding stops, which can play a role in protecting the fetus.
contraception
Used in combination with estrogen to inhibit ovulation in women
Adverse reactions
Occasionally, nausea, vomiting, dizziness, headache, breast swelling and pain, etc. may occur, which may cause fetal genital malformation.
Androgens and anabolic hormones
androgens
Representative medicine
Testosterone, testosterone propionate
Pharmacological effects
Promote the development and maturation of male sexual organs and secondary sexual characteristics. Large doses of androgens can feedbackly inhibit the secretion of gonadotropins and antagonize the effects of estrogen.
It can significantly promote protein synthesis, muscle growth and weight gain. It can also promote the reabsorption of calcium and phosphorus by renal tubules, which is beneficial to bone growth and promotes the reabsorption of water and sodium.
Large doses of androgens can directly stimulate bone marrow hematopoiesis and promote the kidneys to secrete erythropoietin, increasing red blood cell production.
Clinical application
testicular insufficiency
functional uterine bleeding
advanced breast cancer
aplastic anemia
weak
Low-dose androgen treatment can be used to increase the patient's appetite
Adverse reactions
May cause water and sodium retention. Use with caution in patients with nephritis, nephrotic syndrome, hypertension and heart failure.
Long-term use in female patients may lead to masculinization. Once this occurs, the drug should be discontinued immediately.
Anabolic hormone drugs
Representative medicine
Nandrolone phenylpropionate, nandrolone acetate, stanozolol, mestandrolone, etc.
Mainly used for conditions such as insufficient protein absorption, excessive protein decomposition or excessive loss, such as malnutrition, elderly osteoporosis, severe burns, postoperative recovery period and advanced malignant tumors.
When taking medication, the protein content in food should be increased at the same time
birth control pills
female contraceptive pills
Contraceptive pills that mainly inhibit ovulation
Currently the most widespread - short-acting oral contraceptive pills
advantage
Reliable contraceptive effect
Easy to use
Fertility can be restored within a short period of time after discontinuation of medication
Menstruation is normal and has a regulating effect on the menstrual cycle
Pharmacological effects
Suppress ovulation
After large doses of exogenous estrogen and progesterone enter the body, they inhibit the hypothalamic-pituitary system from secreting follicle-stimulating hormone and luteinizing hormone through a negative feedback mechanism, hindering the development and maturation of follicles, thereby inhibiting ovulation.
Change the properties of cervical mucus
Progesterone can reduce cervical mucus secretion, making it thicker and harder for sperm to penetrate into the uterus.
Affect fallopian tube function
Changes the levels of estrogen and progesterone in the normal menstrual cycle, thereby affecting the normal contraction activity of the fallopian tube smooth muscle, changing the running speed of the fertilized egg in the fallopian tube, preventing it from reaching the uterus in time for implantation
Prevent implantation of fertilized egg
A large amount of progesterone can affect the normal proliferation of the endometrium, causing it to shrink and degenerate, which is not conducive to the implantation of a fertilized egg.
Adverse reactions
early pregnancy-like reaction
irregular uterine bleeding
amenorrhea
Hypercoagulation
Can cause increased blood pressure, mild liver damage, and decreased milk production in lactating women.
Anti-pregnancy egg implantation contraceptive pill
Changes in the lining of the uterus, preventing the implantation of the pregnant egg and achieving a contraceptive effect
It is not restricted by the menstrual cycle and is flexible and convenient to use. It can exert a good contraceptive effect if you start taking it on any day. It can be used as an emergency contraceptive measure.
It is suitable for couples living in two places to take it when they visit relatives for a short period of time, so it is called the "Visiting Contraceptive Pill".
Commonly used ones include megestrol, darenolone and anordrin, etc.
external contraceptive pills
There are nonoxynol ether, montelanol ether, alkyl phenyl alcohol ether, etc.
By reducing the surface tension of sperm and damaging the sperm biofilm structure, it kills sperm in the vagina.
Can form mucus to hinder sperm movement and enhance contraceptive effect
It is usually inserted deep into the vagina 5-10 minutes before intercourse.
It has the advantages of easy use, good contraceptive effect, and no obvious adverse reactions.
male contraceptive pill
Gossypol
Through gossypol negative ion radicals and inhibition of NO synthesis, it acts on the seminiferous epithelium of the testicular seminiferous tubules, reducing the number of sperm until there is no sperm.
Gradually recover after stopping medication
Adverse reactions include fatigue, loss of appetite, nausea, vomiting, palpitations and changes in liver function, etc.
Can cause hypokalemia and irreversible spermatogenesis disorders
Drugs that mainly affect uterine and placental functions
Mifepristone and prostaglandin derivatives
It can change the activity of the pregnant uterus, block the inhibitory effect of progesterone on the uterus, or enhance the excitatory effect of prostaglandins on the uterus, increasing uterine activity and terminating pregnancy.
The results of using this type of drug during early pregnancy are equivalent to a normal menstruation.
For anti-early pregnancy and emergency contraception
Adverse reactions mainly include gastrointestinal reactions, severe cases may cause massive bleeding, and medication should be taken under the guidance of a doctor.
Adrenocortical hormone drugs
Glucocorticoids
internal processes
Cortisone and prednisone must be converted into hydrocortisone and prednisolone in the liver to be biologically active. Therefore, patients with severe liver dysfunction should use hydrocortisone or prednisolone.
Pharmacological effects
anti-inflammatory effect
In the early stages of inflammation, it can inhibit local capillary dilation, reduce capillary permeability, and reduce exudation and edema; at the same time, it can inhibit the migration, adhesion, aggregation and phagocytosis of white blood cells, thereby improving redness, swelling, heat, pain, etc. symptom
In the late stage of inflammation, it can significantly inhibit the proliferation of capillaries and fibroblasts, delay the formation of granulation tissue, reduce tissue adhesion, inhibit scar formation, and reduce sequelae.
While glucocorticoids are anti-inflammatory, they also reduce the body's defense function, which can cause the spread of infection and slow wound healing.
anti-immune effects
Small doses inhibit cellular immunity, large doses inhibit humoral immunity
Inhibit the production of allergic mediators and reduce allergic symptoms
antitoxic effect
Improve the body's tolerance to bacterial endotoxins, reduce the release of internal heat sources, inhibit the production of PGE and inhibit the sensitivity of the hypothalamic temperature regulation center to internal heat sources, and have an antipyretic effect on high fever caused by infectious toxemia
It cannot neutralize or destroy botulinum toxin and has no effect against bacterial exotoxins.
Anti-shock effect
Strengthen myocardial contractility, increase cardiac output, reduce the sensitivity of blood vessels to vasoconstrictor substances, expand spasmodic blood vessels, improve microcirculation, stabilize lytic enzyme membranes, and reduce the formation of myocardial inhibitory factors
Other functions
It can stimulate bone marrow hematopoietic function, shorten coagulation time, increase the number of granulocytes, but decrease lymphocytes and eosinophils.
Increase the excitability of the central nervous system, causing euphoria, excitement, insomnia, etc.
Increases the secretion of gastric acid and pepsin, increases appetite, and promotes digestion. However, large doses can induce or aggravate ulcer disease.
Clinical application
alternative therapy
Physiological doses for supplementation in acute and chronic adrenocortical insufficiency, hypopituitarism, and subtotal adrenalectomy
severe infection
Mainly used for patients with toxic infections or shock
While applying sufficient and effective antibacterial drugs, large-dose glucocorticoids can increase the body's tolerance to harmful stimuli, reduce poisoning symptoms, and enable the body to pass the dangerous period.
Viral infections are generally not suitable for use, but for severe viral infections, short-term and large-scale application of glucocorticoids is recommended to relieve symptoms.
Prevent certain inflammatory sequelae
The formation of adhesions and scars in the later stages of inflammation in certain tissues and organs can seriously affect the function of the organs. Early application of glucocorticoids can prevent sequelae.
For non-specific ophthalmia, the application of glucocorticoids can reduce inflammation, relieve pain, and prevent corneal opacity and scar adhesion.
Autoimmune and allergic diseases
autoimmune disease
Comprehensive treatment is usually used, which can significantly relieve symptoms, but cannot cure it.
allergic diseases
This type of drug can be used to treat severe allergic reactions and when other anti-allergic drugs are ineffective.
organ transplant
Combined with other immunosuppressants to inhibit rejection
certain blood diseases
It can be used for aplastic anemia, thrombocytopenia, Henoch-Schonlein purpura, granulocytopenia, acute lymphoblastic leukemia, etc. The effect is not long-lasting and it is easy to relapse after stopping the drug.
Anti-shock
Toxic shock due to infection should be combined with effective and sufficient antibacterial drugs.
For anaphylactic shock, glucocorticoids are the second choice drug, and epinephrine is the first choice. For patients with severe illness, glucocorticoids can be combined with
For hypovolemic shock, when replenishing blood volume or blood transfusion is not effective, super large doses of glucocorticoids can be used together
Topical application
Certain skin diseases have certain curative effects. Hydrocortisone, prednisolone or fluocinolone acetonide are often used.
It can also be used with procaine for local injection for muscle, ligament or joint strain.
Adverse reactions
Caused by long-term large doses
Iatrogenic hyperadrenocorticism-Cushing syndrome
Symptoms may disappear on their own after stopping the drug, and antihypertensive drugs and antidiabetic drugs can be added if necessary.
For long-term use of glucocorticoids, a low-salt, low-sugar, high-protein diet should be given, and potassium supplementation should be paid attention to.
Induce or worsen infection
Long-term use can induce infection or spread potential lesions in the body, aggravating the condition.
Induce or worsen ulcers
It can stimulate the secretion of gastric acid and pepsin, inhibit the secretion of gastric mucus, reduce the resistance of gastrointestinal mucosa to gastric acid, induce or aggravate gastric and duodenal ulcers, and in severe cases can lead to gastrointestinal bleeding and perforation.
cardiovascular system diseases
Due to water and sodium retention and increased blood lipids, high blood pressure and atherosclerosis can occur
other
Inhibits protein synthesis and promotes calcium and phosphorus excretion, leading to muscle atrophy, delayed wound healing, slow development of children, osteoporosis, etc.
Excitable center, mental and behavioral changes, occasional epilepsy and psychotic attacks
Use in the first 3 months of pregnancy may cause fetal malformations
withdrawal reaction
Iatrogenic adrenocortical insufficiency
Long-term use of large amounts of glucocorticoids can cause adrenocortical atrophy and insufficiency
If the drug is stopped suddenly or the drug is reduced too quickly, the patient may suffer from adrenocortical crisis under stress.
Patients who have been taking large amounts of glucocorticoids for a long time should gradually reduce the dosage when stopping the drug. ACTH should be used in combination with ACTH for about 7 days before stopping the drug to promote the recovery of adrenocortical function. When encountering a stressful situation 1 year after stopping the drug, a sufficient amount of glucocorticoids should be given promptly
Rebound phenomenon and withdrawal symptoms
Myalgia, joint pain, myotonia, fever and other symptoms that were not originally present when the drug is suddenly stopped or the dose is reduced too quickly, are called drug withdrawal symptoms.
After the drug is stopped suddenly, symptoms that have been controlled and improved reappear or worsen, which is called rebound phenomenon
It is necessary to increase the dose before treatment, and then stop the drug slowly and reduce the dose after the symptoms improve.
Contraindications
Infections that cannot be controlled by antibiotics, hyperadrenocortical function, recovery from fracture or trauma, recent gastrointestinal anastomosis, corneal ulcers, active peptic ulcers, pregnant women, severe hypertension, diabetes, mental illness and epilepsy, etc.
Usage and treatment course
low dose alternative therapy
Used for chronic adrenal insufficiency, hypopituitarism and postoperative adrenocortical insufficiency
high dose shock therapy
For the treatment of severe infections and anti-shock
After the treatment goal is achieved, the drug can be withdrawn immediately
Typical dose long-term therapy
For the treatment of chronic diseases such as autoimmune diseases
every other day therapy
Give the total dose of the two drugs at 8 a.m. the next day
Mineralocorticoids
Including aldosterone, deoxycorticosterone and corticosterone
Promote Na-K and Na-H exchange in the distal convoluted tubule and collecting duct, retain sodium, retain water, and excrete potassium
Mineralocorticoid secretion is mainly regulated by the renin-angiotensin-aldosterone system composed of plasma and electrolytes.
Treating chronic adrenal insufficiency can correct water and electrolyte disorders and restore water and electrolyte balance.
Overdose can cause water and sodium retention, edema, hypertension, and hypokalemia.
ACTH
ACTH deficiency will cause adrenal cortex atrophy and hyposecretory function, and can also control short-term negative feedback regulation of its own release.
It can only be administered by injection, and hydrocortisone begins to be secreted two hours after administration.
Promote glucocorticoid secretion, but can only exert therapeutic effect when cortical function is intact
Used to diagnose the level of anterior pituitary-adrenocortical function and to discontinue long-term use of glucocorticoids to prevent the development of cortical insufficiency
corticosteroid inhibitors
Mitotan
Pesticide DDT class I compounds
Selectively causes atrophy and necrosis of cells in the zona fasciculata and zona reticularis of the adrenal cortex, but does not affect the zona glomerulosa and aldosterone secretion.
After taking the drug, hydrocortisone and its metabolites in hematuria decreased rapidly.
Mainly used for unresectable cortical cancer, recurrent cancer after resection and postoperative adjuvant treatment of cortical cancer
Metyrapone
For the treatment of hydrocortisone excess and cortical cancer caused by adrenocortical tumors and ACTH-producing tumors
Can be used for functional experiments on gland release ACTH
Aminoglutethimide
Inhibits the synthesis of hydrocortisone and aldosterone
Clinically, it is mainly used in combination with metyrapone to treat Cushing's syndrome induced by excessive secretion of ACTH.
Thyroid hormones and antithyroid drugs
thyroid hormone
drug
Thyroxine T4
Triiodothyronine T3
Pharmacological effects
It can promote protein synthesis and bone growth and development, and is particularly important for the development of the nervous system.
Promote sugar, protein and fat metabolism, promote material oxidation, increase oxygen consumption, improve basal metabolism, and increase heat production
Improve the body's sensitivity to catecholamines, increase the excitability of the central nervous system, accelerate the heart rate, and enhance myocardial contractility, etc.
Clinical application
Mainly used for replacement treatment of hypothyroidism
cretinism
Focus on prevention and early treatment
Myxedema
Start with a small amount and gradually increase to a sufficient amount
simple goiter
Appropriate supplement
Adverse reactions
Overdose may cause symptoms similar to hyperthyroidism. Once this occurs, the drug should be stopped immediately and beta-receptor antagonists should be used if necessary.
antithyroid drugs
Thioureas
Classification
thiouracils
methylthiouracil
propylthiouracil
imidazoles
Methimazole
carbimazole
Pharmacological effects
By combining with peroxidase, it is inactivated, thereby inhibiting the activity of iodine and the coupling process of MlT and DlT, inhibiting the biosynthesis of thyroxine, and having no effect on synthesized thyroid hormone.
Inhibits thyroglobulin production
Propylthiouracil can inhibit the conversion of T4 into T3 in peripheral tissues and can quickly control blood T3 levels.
Clinical application
Medical treatment of hyperthyroidism
Suitable for patients with mild symptoms and those who are not suitable for surgery or radioactive iodine treatment
Give a high dose at the beginning of treatment to maximize the suppression of thyroid hormone synthesis
After 1-3 months of treatment, the symptoms are significantly relieved and the basal metabolic rate is close to normal. The dose can be reduced to the maintenance dose and continued for 1-2 years.
Preparation for hyperthyroidism surgery
Patients who require subtotal thyroidectomy should take thiourea drugs before surgery to restore or close thyroid function to normal, so as to reduce complications after anesthesia and surgery and prevent postoperative thyroid storm.
The use of thioureas will cause gland hyperplasia and tissue congestion, so a large dose of iodine should be used together with it about two weeks before surgery to shrink and harden the glands, making it easier for surgery.
Adjuvant treatment for thyroid storm
High-dose iodine is used to inhibit the release of thyroid hormones, and high-dose (twice the therapeutic amount) thioureas can be used to block the synthesis of thyroid hormones as auxiliary treatment. Propylthiouracil is often preferred
Adverse reactions
allergic reaction
Agranulocytosis—serious adverse reactions
Blood pictures should be checked regularly and medication should be discontinued immediately if any
Hepatotoxicity
Propylthiouracil can cause hepatocellular damage, and use of methimazole can cause obstructive jaundice
goiter
hypothyroidism
Check regularly. Pregnant women should use with caution. Breastfeeding should be stopped during lactation.
Iodine and iodide
Representative medicine
Potassium iodide, sodium iodide, compound iodine solution
Pharmacological effects
Small doses of iodine are involved in the synthesis of thyroid hormones
High doses of iodine produce antithyroid effects
Inhibit proteolytic enzymes, preventing T3 and T4 from dissociating from thyroglobulin and reducing their release
Inhibits peroxidase and affects thyroid hormone synthesis
Antagonize the effects of TSH
Clinical application
Prevent and treat simple goiter
Preparation for hyperthyroidism surgery
thyroid storm
Adverse reactions
Mainly caused by acute allergic reactions, angioedema, upper respiratory tract congestion and severe laryngeal edema may also occur, which can cause suffocation.
Long-term medication has the risk of inducing hypothyroidism and aggravating the symptoms of hyperthyroidism
radioactive iodine
131-I
Half-life is about 8 days
Pharmacological effects
The range is 0.5-2mm, and its radiation effect is limited to the thyroid parenchyma, which can cause effects similar to the removal of part of the thyroid gland.
It can be measured in vitro and can be used to determine the iodine uptake function of the thyroid gland.
Clinical application
Hyperthyroidism
Only used for those who are not susceptible to surgery or have recurrence after surgery and are ineffective or allergic to thiourea.
Thyroid function test
Adverse reactions
Excessive dosage may lead to hypothyroidism
beta receptor antagonists
Sympathetic nerve activity is enhanced in patients with hyperthyroidism. By blocking β2 receptors on the presynaptic membrane of adrenergic nerves, it inhibits positive feedback regulation, reduces the release of norepinephrine, and antagonizes the effects of catecholamines.
Control symptoms such as tachycardia, excessive sweating, hand tremors, and anxiety in patients with hyperthyroidism
As an adjuvant therapy for hyperthyroidism and thyroid storm
It does not interfere with the effect of thiourea drugs on the thyroid gland and acts rapidly. It can be combined with thiourea drugs to enhance the efficacy.
It is suitable for patients with hyperthyroidism who are not suitable for other antithyroid drugs, surgery and I-131 treatment.
It is also used to prepare for thyroid surgery, which can make the gland less likely to tear and facilitate surgery.
Insulin and oral hypoglycemic drugs
insulin
Classification characteristics
Ultra short acting
insulin lispro
Immediately before meal
short acting
regular insulin
Ketosis coma first aid
Half an hour before meals, the dosage depends on the condition
Medium effect
low protamine zinc insulin
Inject once half an hour before breakfast, and if necessary, add once before dinner. The dose depends on the condition.
Long lasting
protamine zinc insulin
1 hour before breakfast or dinner
Pharmacological effects
Glucose metabolism
fat metabolism
protein metabolism
Promote k transport
Clinical application
type 1 diabetes
Type 2 diabetes that cannot be controlled by diet control and oral hypoglycemic drugs
People with various acute or severe complications of diabetes, such as ketoacidosis and non-ketotic hyperosmolar coma
Various types of diabetes combined with severe infection, wasting disease, high fever, pregnancy, trauma and surgery
Correct intracellular potassium deficiency
Combined with potassium chloride and glucose to form a polarizing solution, it is used to prevent and treat arrhythmias in myocardial infarction or other heart diseases.
Adverse reactions
hypoglycemia
Generally, those with mild symptoms can drink sugar water, while those with severe symptoms should immediately inject 50% glucose intravenously.
allergic reaction
Insulin resistance
lipoatrophy
Oral hypoglycemic drugs
Sulfonylureas
Representative medicine
tolbutamide
chlorpropamide
glyburide
Glipizide
Glezite
Pharmacological effects
Hypoglycemic
It can reduce blood sugar in normal people and diabetic patients with still functioning pancreatic islet function, but it is useless for type 1 diabetic patients and those who have had their pancreas removed. Poor efficacy in patients with severe diabetes
Gliclazide is an anti-thrombotic agent
antidiuretic
Glibenclamide and cyclopropamide can be used for diabetes insipidus
Mechanism
Mainly by stimulating the release of insulin from pancreatic beta cells, it can also reduce insulin metabolism, increase the sensitivity of surrounding tissues to insulin, increase the binding of insulin to its receptors, and inhibit glucagon secretion.
Clinical application
For patients with type 2 diabetes whose islet function remains and cannot be controlled by diet alone.
Glibenclamide and cyclopropamide can significantly reduce the patient's urine output, and their combined use with thiazides can improve the efficacy.
Adverse reactions
digestive tract reaction
Blood and liver function needs to be checked regularly
persistent hypoglycemia
Chlorpropamide can cause central nervous system symptoms
Not suitable for use in the elderly and diabetic patients with poor renal function
Biguanides
Take with or after meals
Metformin
Promote the uptake and utilization of glucose in surrounding adipose tissue, promote anaerobic glycolysis of sugar in muscle tissue, inhibit glucose absorption and gluconeogenesis in the intestine, and inhibit the release of glucagon
Significantly lowers the blood sugar levels of diabetic patients with preserved or complete loss of pancreatic islet function, but has no effect on the blood sugar of normal people.
Mainly used for patients with type 2 diabetes, especially those who are obese, overweight and those who cannot be controlled by diet alone.
Gastrointestinal reactions are more common in the early stages of medication
Metformin generally does not cause lactic acidemia, compared with phenformin
phenformin
alpha-glucosidase inhibitor
Acarbose
Can competitively inhibit small intestinal α-glucosidase, reduce glucose absorption, thereby lowering postprandial blood sugar
It is clinically used to treat type 2 diabetes, especially for diabetic patients with normal fasting blood sugar but significantly elevated postprandial blood sugar.
Mainly gastrointestinal reactions, hypoglycemic reactions may occur in some cases
Voglibose
Miglitol
Meal blood sugar regulator
Taken with meals, it is used for patients with type 2 diabetes. It is especially suitable for postprandial hyperglycemia and can prevent cardiovascular complications of diabetes.
repaglinide
It is suitable for postprandial blood sugar increase in type 2 diabetes, elderly diabetes and diabetic nephropathy. It can be used in combination with biguanide drugs to enhance the efficacy.
Can increase weight
Naglina
Miglinel
insulin sensitizer
After meal, between meals
Thiazolidinediones
Representative medicine
Rosiglitazone
pioglitazone
ciglitazone
Emglitazone
Mechanism
Enhance the sensitivity of target tissues to insulin to improve insulin resistance, lower blood sugar, improve lipid metabolism disorders, etc.
Clinical application
Type 2 diabetes in whom other hypoglycemic drugs are ineffective, especially those with insulin resistance
Adverse reactions
Lethargy
weight gain, edema
Muscle pain, bone pain, headache
Patients with active liver disease and heart disease should not use it. Regularly monitor liver function during use.
Other new hypoglycemic drugs
dipeptidyl peptidase-4 inhibitor
Representative drugs - sitagliptin, saxagliptin, vildagliptin
By selectively inhibiting DPP-4, it enhances insulin secretion and inhibits glucagon secretion to lower blood sugar.
It can effectively reduce fasting blood sugar and postprandial blood sugar without increasing the risk of hypoglycemia or weight gain.
glucagon-like peptide-1 receptor agonist
Representative drugs-exenatide and liraglutide, both require subcutaneous injection
By stimulating GLP-1 receptors, it inhibits the secretion of glucagon from pancreatic islet A cells, suppresses appetite, and delays content emptying.
Suitable for obese diabetic patients
Common gastrointestinal reactions, mainly seen during initial treatment
Sodium-glucose cotransporter 2 inhibitor
Representative drugs-canagliflozin, dapagliflozin
By inhibiting glucose reabsorption in the proximal renal tubule, glucose is excreted in the urine, thereby lowering blood glucose levels regardless of insulin.
In addition to the hypoglycemic effect, it can also reduce weight and lower blood pressure.
Suitable for patients with type 2 diabetes who have poor blood sugar control through diet and exercise
No hypoglycemia reaction, dizziness, hypotension, polyuria and other reactions may occur occasionally
amylin analogs
pramlintide
It can delay the absorption of glucose, inhibit glucagon secretion, and reduce liver glycogen production, thereby lowering blood sugar in diabetic patients.
Mainly used for diabetic patients who are ineffective on insulin alone or combined with sulfonylureas or biguanides.
Adverse reactions include hypoglycemia, gastrointestinal reactions, joint pain, headache, dizziness, fatigue, etc.
Drugs that affect other metabolism
Calcium and phosphorus metabolism regulating drugs
Bisphosphonates
alendronate
calcitonin
salmon calcitonin
Vitamin D and its derivatives
Calcitriol
Can be used for bone diseases caused by reduced osteotriol
High-dose intravenous administration for secondary hyperparathyroidism due to renal failure
Hypercalcemia and hypercalciuria caused by overdose
Calcium preparations
Estrogens
It can reduce bone resorption in elderly women who have suffered vertebral compression fractures and delay the development of osteoporosis, but it cannot restore the bone texture to normal.
Weight loss pills
appetite suppressant
Representative medicine
Fenfluramine, dexfenfluramine, phentermine, bupropion
Act on the central nervous system
Adverse reactions causing myocardial valvular disease
metabolism enhancer
Thyroxine preparations
5-HT and norepinephrine reuptake inhibitors
Western Quming
Can increase serious cardiovascular risk, production, sales and use have been stopped
lipase inhibitor
Inactivate gastrointestinal esterase to reduce triglycerides, absorb them in the intestine, and reduce energy intake
orlistat
The only OTC weight loss drug currently available
For long-term treatment of obese and overweight patients who have implemented moderate diet control and exercise, including patients who have developed obesity-related risk factors.
The main adverse reaction is gastrointestinal reaction
Contraindicated in patients with chronic malabsorption syndrome and cholestasis