2.Endocrine Pharmacology.docx
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Medical University of Plovdiv
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+-------------+-------------+-------------+-------------+-------------+ | **PITUITARY | | | | | | /HYPOTHALAM | | | | | | IC | | | | | | PHARMACOLO...
+-------------+-------------+-------------+-------------+-------------+ | **PITUITARY | | | | | | /HYPOTHALAM | | | | | | IC | | | | | | PHARMACOLOG | | | | | | Y** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Leuprolid | | | | | | e** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Gonadotr | \- | | \- Symptoms | | | opin-Releas | Endometrios | | of | | | ing | is | | hypogonadis | | | Hormone | (Continuous | | m | | | (GnRH) | admin) | | | | | Receptor | | | \- Bone | | | Agonist]{.u | \- | | pain | | | nderline}** | Leiomyomas | | | | | | (Uterine | | \- Feet | | | \- GnRH is | fibroids) | | swelling | | | normally | | | | | | secreted in | \- | | \- Ankle | | | a pulsatile | Amenorrhea | | swelling | | | fashion by | (Pulsatile | | | | | the | admin) | | | | | hypothalamu | | | | | | s | \- Prostate | | | | | and | cancer | | | | | stimulates | | | | | | the release | \- Breast | | | | | of **FSH** | cancer | | | | | and **LH** | | | | | | from the | | | | | | **anterior | | | | | | pituitary | | | | | | gland** | | | | | | ultimately | | | | | | leading to | | | | | | increased | | | | | | serum | | | | | | **oestradio | | | | | | l** | | | | | | and | | | | | | **testoster | | | | | | one** | | | | | | levels via | | | | | | the normal | | | | | | physiology | | | | | | of the | | | | | | **hypothala | | | | | | mic--pituit | | | | | | ary--gonada | | | | | | l | | | | | | axis (HPG | | | | | | axis)** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Somatotro | | | | | | pin | | | | | | (Growth | | | | | | Hormone | | | | | | analogue)** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Growth | \- Dwarfism | | \- | | | Hormone | | | Hand/foot | | | analogue:]{ | \- Muscle | | oedema | | |.underline} | waste | | | | | ** | related to | | \- | | | | AIDS/malign | | Arthralgias | | | **Binds** | ancy | | | | | to the | | | \- Carpal | | | growth | | | Tunnel | | | hormone | | | Syndrome | | | **receptor* | | | | | | * | | | \- | | | expressed | | | Decreased | | | in **target | | | Insulin | | | cells** in | | | Sensitivity | | | the | | | | | | **liver** | | | \- | | | and | | | Hyperglycae | | | **cartilage | | | mia | | | ** | | | | | | to | | | | | | **stimulate | | | | | | intracellul | | | | | | ar | | | | | | processes** | | | | | | for | | | | | | increasing | | | | | | bone | | | | | | growth, | | | | | | increasing | | | | | | bone mass, | | | | | | increasing | | | | | | muscle and | | | | | | reduced fat | | | | | | mass, and | | | | | | regulating | | | | | | blood | | | | | | glucose and | | | | | | lipid | | | | | | levels | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Octreotid | | | | | | e | | | | | | (**Somatost | | | | | | atin | | | | | | analogue) | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Somatost | \- | | \- | | | atin | Oesophageal | | Gallbladder | | | Analogue]{. | varices | | disease | | | underline}* | | | | | | * | \- VIPomas | | \- | | | | | | Pancreatiti | | | Inhibits | \- | | s | | | secretion | Carcinoid | | | | | of many | syndrome | | \- | | | hormones | | | Hypo-thyroi | | | including | \- | | dism | | | **GH**, | Acromegaly | | | | | **glucagon* | | | \- | | | * | \- | | Hyper-thyro | | | and | Zollinger-E | | idism | | | **insulin** | llison | | | | | by binding | | | \- | | | predominant | Syndrome | | Hypo-glycae | | | ly | | | mia | | | to the | | | | | | somatostati | | | \- | | | n | | | Hyper-glyca | | | receptors | | | emia | | | **SSTR2** | | | | | | and | | | | | | **SSTR5**. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Dopamine | | | | | | Agonists** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Dopamine | \- | | \- | \- | | receptor | Prolactinom | | Psychotic | Bromo.cript | | agonists.]{ | as | | symptoms | ine | |.underline} | | | | | | ** | \- | | \- | \- | | | Parkinson | | Dizziness | Caber.golin | | \- Dopamine | disease | | | e | | inhibits | | | \- Headache | | | prolactin | (High doses | | | | | secretion. | required) | | \- Nausea | | | | | | | | | | | | \- | | | | | | Light-heade | | | | | | dness | | | | | | | | | | | | \- | | | | | | Confusion | | +-------------+-------------+-------------+-------------+-------------+ | **Desmopres | | | | | | sin** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Vasopres | \- Central | | \- | | | sin | Diabetes | | Hyponatremi | | | analogue | Insipidus | | a, | | | (ADH)]{.und | | | | | | erline}** | \- | | \- | | | | Haemophilia | | Transient | | | \- | A | | headache, | | | Primarily | | | | | | effects on | \- Von | | \- Flushing | | | **V2 | Willebrand | | | | | receptors** | Disease | | | | | (located in | | | | | | renal | | | | | | tubules to | | | | | | increase | | | | | | water | | | | | | reabsorptio | | | | | | n). | | | | | | Also | | | | | | stimulates | | | | | | release of | | | | | | **von | | | | | | Willebrand | | | | | | factor | | | | | | (vWF)** | | | | | | from the | | | | | | endothelium | | | | | | which | | | | | | function | | | | | | for | | | | | | platelet | | | | | | aggregation | | | | | |. | | | | | | | | | | | | Has | | | | | | **minimal** | | | | | | V1 activity | | | | | | (located on | | | | | | vascular | | | | | | | | | | | | smooth | | | | | | muscle | | | | | | providing | | | | | | vasoconstri | | | | | | ctive | | | | | | effect). | | | | | +-------------+-------------+-------------+-------------+-------------+ | **ADH | | | | | | Antagonists | | | | | | ** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Conivapt | \- | | \- | \- | | an | Hyponatremi | | Hypernatrem | Demeclocycl | | and | a | | ia | ine | | Tolvaptan]{ | due to | | | | |.underline} | SIADH, | | \- | \- | | ** | | | Hypokalaemi | Conivaptan | | | \- | | a | | | \- Inhibit | Congestive | | | \- | | ADH | heart | | \- | Tolvaptan | | receptors | failure | | Hypotension | | | (V 1 and | | | | | | V2) | \- Liver | | | | | directly, | cirrhosis | | | | | | | | | | | **[Demecloc | | | | | | ycline]{.un | | | | | | derline}** | | | | | | | | | | | | \- inhibits | | | | | | the second | | | | | | messenger | | | | | | cascade | | | | | | through an | | | | | | unknown | | | | | | mechanism | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Oxytocin* | | | | | | * | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Contraind | **Side | **Examples* | | of Action** | Use** | ications** | Effects** | * | +-------------+-------------+-------------+-------------+-------------+ | Posterior | | | \- Chest | | | pituitary | | | pain | | | hormone | | | | | | that | | | \- | | | stimulates | | | Confusion | | | milk | | | | | | secretion | | | \- | | | and induces | | | Excessive | | | uterine | | | vaginal | | | contraction | | | bleeding | | | s | | | | | | during | | | \- | | | labour. | | | Palpitation | | | | | | s | | | | | | | | | | | | \- Seizure | | +-------------+-------------+-------------+-------------+-------------+ | **Insulin | | | | | | Preparation | | | | | | s** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Bind | | \- | | **[Rapid-Ac | | insulin | | Hypoglycaem | | ting]{.unde | | receptor | | ia | | rline}** | | (tyrosine | | | | | | kinase | | \- | | \- Lispro | | activity)]{ | | Lipodystrop | | | |.underline} | | hy | | \- Aspart | | ** | | | | | | | | \- | | \- | | [Liver:]{.u | | Hypersensit | | Glu.lisine | | nderline} | | ivity | | | | | | | | **[Short-Ac | | \- | | \- Weight | | ting]{.unde | | Increases | | gain | | rline}** | | glucose | | | | | | storage as | | | | \- Regular | | glycogen | | | | | | | | | | **[Intermed | | [Muscle:]{. | | | | iate-Acting | | underline} | | | | ]{.underlin | | | | | | e}** | | \- | | | | | | Increases | | | | \- NPH | | glycogen | | | | | | and protein | | | | **[Long | | synthesis | | | | Acting]{.un | | | | | | derline}** | | [Fat: | | | | | | ]{.underlin | | | | \- Detemir | | e} | | | | | | | | | | \- Glargine | | \- | | | | | | Increases | | | | **[Very | | TG storage | | | | Long | | | | | | Acting]{.un | | \- Insulin | | | | derline}** | | facilitates | | | | | | both | | | | \- Degludec | | glucose | | | | | | uptake and | | | | | | triglycerid | | | | | | e | | | | | | storage. | | | | | | | | | | | | [Cell | | | | | | Membrane:]{ | | | | | |.underline} | | | | | | | | | | | | \- | | | | | | Indirectly | | | | | | causes K+ | | | | | | uptake | | | | | | alongside | | | | | | glucose | | | | | | uptake. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Metformin | | | | | | - Increase | | | | | | Insulin | | | | | | Sensitivity | | | | | | ** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | [Inhibits | | \- G.I. | \- Renal | | | Gluconeogen | | upset | insufficien | | | esis | | | cy | | | ]{.underlin | | \- Lactic | | | | e} | | acidosis | | | | | | (Use with | | | | Inhibits | | caution in | | | | **mitochond | | renal | | | | rial | | insufficien | | | | glycerol-3- | | cy) | | | | phosphate** | | | | | | | | \- Vitamin | | | | **dehydroge | | B12 | | | | nase | | deficiency | | | | (mGPD)**, | | | | | | essential | | \- Weight | | | | in | | loss | | | | gluconeogen | | | | | | esis, | | | | | | | | | | | | [Inhibits | | | | | | Glucagon]{. | | | | | | underline} | | | | | | | | | | | | It also | | | | | | inhibits | | | | | | the effects | | | | | | of | | | | | | glucagon, | | | | | | which | | | | | | increases | | | | | | blood | | | | | | sugar. Also | | | | | | increases | | | | | | glycolysis | | | | | | and insulin | | | | | | receptor | | | | | | sensitivity | | | | | | via | | | | | | activation | | | | | | of special | | | | | | enzyme. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Pio.glita | | | | | | zone | | | | | | - Increase | | | | | | Insulin | | | | | | Sensitivity | | | | | | ** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | \- Activate | | \- Weight | - Glimepi | Pio.glitazo | | **PPAR-γ (a | | gain | ride | ne | | nuclear | | | | | | receptor)** | | \- Oedema | | | | , | | | | | | which | | \- Heart | | | | initiates | | failure | | | | intracellul | | | | | | ar | | \- Higher | | | | gene | | risk | | | | modulation | | fractures | | | | to increase | | | | | | sensitivity | | \- Delayed | | | | of insulin | | onset of | | | | receptors, | | action | | | | which | | (weeks) | | | | increases | | | | | | glucose | | | | | | uptake from | | | | | | blood, | | | | | | decreasing | | | | | | blood sugar | | | | | | levels. | | | | | | | | | | | | \- Also | | | | | | increases | | | | | | **adiponect | | | | | | in**, | | | | | | a protein | | | | | | secreted by | | | | | | adipose | | | | | | tissue to | | | | | | improves | | | | | | **glucose | | | | | | metabolism* | | | | | | * | | | | | | and **fatty | | | | | | acid | | | | | | storage** | | | | | | (circulatin | | | | | | g | | | | | | fatty acids | | | | | | risks | | | | | | insulin | | | | | | resistance) | | | | | |. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Sul.fonyl | | | | | |.ureas | | | | | | and | | | | | | Meg.lit.ini | | | | | | des** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | **[Increase | | **[Sulfonyl | \- Renal | **[Sulfonyl | | insulin | | ureas | insufficien | ureas | | secretion]{ | | (1stG)]{.un | cy | (1stG)]{.un | |.underline} | | derline}** | increases | derline}** | | ** | | | risk of | | | | | \- | hypoglycaem | \- | | Close K+ | | Disulfiram- | ia | Chlorpropam | | channels in | | like | | ide | | pancreatic | | reactions | | | | B cell | | | | \- | | | | \- | | Tolbutamide | | membrane | | Hypoglycaem | | | | causing | | ia | | **[Sulfonyl | | cell | | | | ureas | | depolarizat | | \- Weight | | (2ndG)]{.un | | ion | | gain | | derline}** | | which leads | | | | | | to opening | | | | \- | | of calcium | | | | Glipizide | | channels | | | | | | and influx | | | | \- | | of calcium | | | | Glyburide | | ions which | | | | | | cause | | | | **[Meglitin | | release of | | | | ides]{.unde | | intracellul | | | | rline}** | | ar | | | | | | insulin | | | | \- | | stores. | | | | Nateglinide | | | | | | | | | | | | \- | | | | | | Repaglinide | +-------------+-------------+-------------+-------------+-------------+ | **GLP-1 | | | | | | analogues - | | | | | | "glutide"** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Glucagon-li | | \- Nausea | | \- | | ke | | | | Exena.tide | | peptide-1 | | \- Vomiting | | | | (GLP-1) is | | | | \- | | a hormone | | \- | | Lira.glutid | | that is | | Pancreatiti | | e | | naturally | | s | | | | produced in | | | | \- | | the | | \- Weight | | Sema.glutid | | intestines | | loss | | e | | to regulate | | | | | | glucose | | \- | | | | metabolism. | | Increased | | | | | | satiation | | | | **[Decrease | | | | | | s | | | | | | Glucagon | | | | | | Release]{.u | | | | | | nderline}** | | | | | | | | | | | | \- Inhibit | | | | | | the release | | | | | | of glucagon | | | | | | from | | | | | | pancreatic | | | | | | alpha | | | | | | cells. | | | | | | | | | | | | **[Decrease | | | | | | Gastric | | | | | | Emptying]{. | | | | | | underline}* | | | | | | * | | | | | | | | | | | | \- Control | | | | | | the | | | | | | postprandia | | | | | | l | | | | | | (after-meal | | | | | | ) | | | | | | rapid rise | | | | | | in blood | | | | | | glucose | | | | | | levels | | | | | | | | | | | | **[Glucose- | | | | | | Dependent | | | | | | Insulin | | | | | | Release]{.u | | | | | | nderline}** | | | | | | | | | | | | \- | | | | | | Stimulate | | | | | | insulin | | | | | | secretion | | | | | | only when | | | | | | blood | | | | | | glucose | | | | | | levels are | | | | | | elevated. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **DPP-4 | | | | | | inhibitors | | | | | | "gliptin"** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Inhibits | | \- | | \- | | **Dipeptidy | | Respiratory | | Lina.glipti | | l | | Infections | | n | | peptidase-4 | | | | | | (DPP-4) | | \- Urinary | | \- | | enzyme** | | Infections | | Saxa.glipti | | that | | | | n | | **deactivat | | \- No | | | | es | | effect on | | \- | | Glucagon-li | | weight | | Sita.glipti | | ke | | | | n | | peptide-1 | | \- | | | | (GLP-1) | | Increased | | | | (incretin)* | | satiety | | | | * | | | | | | and | | | | | | inhibiting | | | | | | its | | | | | | positive | | | | | | effects of | | | | | | glucose | | | | | | regulation. | | | | | | | | | | | | [Decreases | | | | | | Glucagon | | | | | | Release]{.u | | | | | | nderline} | | | | | | | | | | | | \- Inhibit | | | | | | the release | | | | | | of glucagon | | | | | | from | | | | | | pancreatic | | | | | | alpha | | | | | | cells. | | | | | | | | | | | | [Decrease | | | | | | Gastric | | | | | | Emptying]{. | | | | | | underline} | | | | | | | | | | | | \- Control | | | | | | the | | | | | | postprandia | | | | | | l | | | | | | (after-meal | | | | | | ) | | | | | | rapid rise | | | | | | in blood | | | | | | glucose | | | | | | levels | | | | | | | | | | | | [Increased | | | | | | Glucose-Dep | | | | | | endent | | | | | | Insulin | | | | | | Release]{.u | | | | | | nderline} | | | | | | | | | | | | \- | | | | | | Stimulate | | | | | | insulin | | | | | | secretion | | | | | | when eating | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Sodium-Gl | | | | | | ucose | | | | | | Co-transpor | | | | | | ter | | | | | | 2 | | | | | | Inhibitors | | | | | | "gliflozin" | | | | | | ** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | | **Side | **Contraind | **Examples* | | of Action** | | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | **Block** | | \- | \- Use with | \- | | the | | Glucosuria | caution in | Cana.gliflo | | reabsorptio | | | renal | zin | | n | | (UTIs, | insufficien | | | of glucose | | vulvovagina | cy | \- | | in the | | l | | Dapa.gliflo | | **proximal | | candidiasis | (Decreased | zin | | convoluted | | ) | efficacy | | | tubules** | | | with | \- | | of the | | \- | decreased | Empa.gliflo | | kidneys and | | Dehydration | GFR). | zin | | **increase | | | | | | urinary | | (Orthostati | | | | glucose | | c | | | | excretion.* | | hypotension | | | | * | | ) | | | | In a normal | | | | | | state, most | | \- Weight | | | | of the | | loss | | | | filtered | | | | | | glucose is | | | | | | reabsorbed | | | | | | back into | | | | | | the | | | | | | bloodstream | | | | | | from the | | | | | | renal | | | | | | tubules. | | | | | | This | | | | | | reabsorptio | | | | | | n | | | | | | is | | | | | | facilitated | | | | | | by | | | | | | **SGLT2**, | | | | | | a protein | | | | | | located in | | | | | | the | | | | | | proximal | | | | | | convoluted | | | | | | tubules of | | | | | | the kidneys | | | | | +-------------+-------------+-------------+-------------+-------------+ | **α-Glucosi | | | | | | dase | | | | | | Inhibitors* | | | | | | * | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Work by | | \- GI upset | \- Renal | \- Acarbose | | **inhibitin | | | insufficien | | | g** | | \- Bloating | cy | \- Miglitol | | the action | | | | | | of the | | | | | | enzyme | | | | | | **α-glucosi | | | | | | dase**, | | | | | | which plays | | | | | | a role in | | | | | | the | | | | | | **digestion | | | | | | and | | | | | | absorption | | | | | | of | | | | | | carbohydrat | | | | | | es** | | | | | | in the | | | | | | small | | | | | | intestine. | | | | | | By | | | | | | inhibiting | | | | | | this | | | | | | enzyme, | | | | | | α-glucosida | | | | | | se | | | | | | inhibitors | | | | | | **slow down | | | | | | the | | | | | | hydrolysis | | | | | | and | | | | | | absorption | | | | | | of | | | | | | carbohydrat | | | | | | es**, | | | | | | resulting | | | | | | in a | | | | | | reduction | | | | | | in | | | | | | postprandia | | | | | | l | | | | | | (after-meal | | | | | | ) | | | | | | blood sugar | | | | | | levels. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Amylin | | | | | | analogues** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Amylin, a | | \- | | Pram.lintid | | hormone | | Hypoglycaem | | e | | that is | | ia | | | | **co-secret | | | | | | ed | | \- Nausea | | | | with | | | | | | insulin** | | \- | | | | by the | | Increased | | | | **beta | | satiety | | | | cells** in | | | | | | the | | | | | | pancreas. | | | | | | | | | | | | [Decreases | | | | | | Glucagon | | | | | | Release]{.u | | | | | | nderline} | | | | | | | | | | | | \- Inhibit | | | | | | the release | | | | | | of glucagon | | | | | | from | | | | | | pancreatic | | | | | | alpha | | | | | | cells. | | | | | | | | | | | | [Decrease | | | | | | Gastric | | | | | | Emptying]{. | | | | | | underline} | | | | | | | | | | | | \- Control | | | | | | the | | | | | | postprandia | | | | | | l | | | | | | (after-meal | | | | | | ) | | | | | | rapid rise | | | | | | in blood | | | | | | glucose | | | | | | levels. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Thionamid | | | | | | es** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Hyperthyroi | \- | \- Skin | [Methimazol | \- | | dism | Hyperthyroi | rash | e]{.underli | Methimazole | | can | dism | | ne} |. | | increase | | \- | | | | gluconeogen | \- | Agranulocyt | \- 1^st^ | \- | | esis | Methimazole | osis | trimester | Propylthiou | | and | (2nd/3^rd^ | | of | racil | | glycolysis, | trimester) | \- Aplastic | pregnancy | | | both | | anaemia | due to | | | leading to | \- PTU | | teratogenic | | | increased | (1^st^ | \- | ity | | | blood sugar | trimester) | Hepatotoxic | | | | levels. | | ity | [Propylthio | | | Thionamides | | | uracil]{.un | | | block | | [Propylthio | derline} | | | thyroid | | uracil]{.un | | | | peroxidase, | | derline} | \- 2/3^rd^ | | | inhibiting | | | trimester | | | the | | \- | of | | | oxidation | | ANCA-positi | pregnancy | | | of iodide | | ve | (due to | | | as well as | | vasculitis | hepatotoxic | | | the | | | ity) | | | organificat | | [Methimazol | | | | ion | | e]{.underli | | | | and | | ne} | | | | coupling of | | | | | | iodine, | | \- | | | | **preventin | | Teratogen | | | | g | | | | | | the | | | | | | synthesis | | | | | | of thyroid | | | | | | hormones**. | | | | | | | | | | | | [Propylthio | | | | | | uracil | | | | | | (PTU)]{.und | | | | | | erline} | | | | | | | | | | | | Also | | | | | | **blocks | | | | | | 5′-deiodina | | | | | | se** | | | | | | which is | | | | | | responsible | | | | | | for | | | | | | converting | | | | | | T4 to T3 in | | | | | | periphery. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Levothyro | | | | | | xine | | | | | | and | | | | | | Liothyronin | | | | | | e** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | **Examples* | | of Action** | Use** | Effects** | ications** | * | +-------------+-------------+-------------+-------------+-------------+ | Levothyroxi | \- | \- | [Levothyrox | [Misused | | ne | Hypothyroid | Tachycardia | ine]{.under | for weight | | (synthetic | ism | | line} | loss]{.unde | | T4) | | \- Heat | | rline} | | | \- | intolerance | \- Antacids | | | Liothyronin | Myxoedema | | | \- TSH | | e | | \- Tremor | \- Bile | Receptor | | (synthetic | \- Weight | | acid resins | antibody | | T3) | loss | \- | | test | | | | Arrhythmias | \- Ferrous | | | | | | sulphate | Radioactive | | | | | | Iodine | | | | | | Uptake | | | | | | | | | | | | \- Thyroid | | | | | | blood flow | | | | | | on U/S | +-------------+-------------+-------------+-------------+-------------+ | **Fludrocor | | | | | | tisone | | | | | | (aldosteron | | | | | | e | | | | | | analogue)** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | | | of Action** | Use** | Effects** | ications** | | +-------------+-------------+-------------+-------------+-------------+ | Synthetic | \- | \- Retains | | | | analogue of | Mineralocor | fluid | | | | aldosterone | ticoid | (oedema) | | | | (mineraloco | replacement | | | | | rticoid) | in 1° | \- | | | | with | adrenal | Exacerbatio | | | | glucocortic | insufficien | n | | | | oid | cy. | of heart | | | | effects. | | failure | | | | Aldosterone | | | | | | acts on the | | \- | | | | distal | | Hyperpigmen | | | | tubules and | | tation | | | | collecting | | | | | | ducts of | | | | | | the | | | | | | kidneys, | | | | | | where it | | | | | | promotes | | | | | | the | | | | | | reabsorptio | | | | | | n | | | | | | of sodium | | | | | | ions (Na+) | | | | | | from the | | | | | | filtrate | | | | | | back into | | | | | | the | | | | | | bloodstream | | | | | |. | | | | | | In | | | | | | Addison's | | | | | | disease the | | | | | | adrenal | | | | | | cortex | | | | | | failure to | | | | | | synthesize | | | | | | enough | | | | | | aldosteroni | | | | | | sm. | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Cinacalce | | | | | | t** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | | | of Action** | Use** | Effects** | ications** | | +-------------+-------------+-------------+-------------+-------------+ | Binds to | \- 2^nd^ | \- | | | | and | Hyperparath | Hypocalcemi | | | | **activates | yroidism | a | | | | calcium-sen | (CKD | | | | | sing | patients on | | | | | receptor | haemodialys | | | | | (CaSR)** in | is) | | | | | **parathyro | | | | | | id | \- | | | | | gland**, | Hypercalcem | | | | | where Ca2+ | ia | | | | | would | (associated | | | | | typically | with 1^st^ | | | | | bind to, | hyperparath | | | | | giving the | yroidism) | | | | | effect of | | | | | | sufficient | \- | | | | | circulating | Parathyroid | | | | | calcium | carcinoma | | | | | ions in | | | | | | serum to | | | | | | **calcium-s | | | | | | ensing | | | | | | receptors | | | | | | (CaSR)** | | | | | | located in | | | | | | parathyroid | | | | | | gland, so | | | | | | they | | | | | | **decrease | | | | | | parathyroid | | | | | | hormone | | | | | | synthesis.* | | | | | | * | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Sevelamer | | | | | | ** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | | | of Action** | Use** | Effects** | ications** | | +-------------+-------------+-------------+-------------+-------------+ | Non-absorba | \- | \- | | | | ble | Hyperphosph | Hypophospha | | | | **phosphate | atemia | temia | | | | binder** | in CKD | | | | | that | | \- GI upset | | | | prevents | | | | | | phosphate | | | | | | absorption | | | | | | from the GI | | | | | | tract | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Cation | | | | | | exchange | | | | | | resins** | | | | | +-------------+-------------+-------------+-------------+-------------+ | **Mechanism | **Clinical | **Side | **Contraind | | | of Action** | Use** | Effects** | ications** | | +-------------+-------------+-------------+-------------+-------------+ | These | \- | \- | | \- | | resins work | Hyperkalaem | Hypokalaemi | | Patiromer | | by | ia | a | | | | **binding | | | | \- Sodium | | to | | \- GI upset | | | | potassium | | | | \- | | ions** in | | | | Polystyrene | | the | | | | | | gastrointes | | | | \- | | tinal | | | | Sulfonate, | | tract, | | | | | | preventing | | | | \- | | their | | | | Zirconium | | absorption | | | | | | into the | | | | \- | | bloodstream | | | | Cyclosilica | | and | | | | te | | facilitatin | | | | | | g | | | | | | their | | | | | | excretion | | | | | | from the | | | | | | body | | | | | | through the | | | | | | stool. | | | | | +-------------+-------------+-------------+-------------+-------------+