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47 Cards in this Set
- Front
- Back
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mineralocorticoids gen
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mineralocorticoids:
- natural: aldosterone - main action: Na retention, K excretion |
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mineralocorticoids mechanism
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mineralocorticoids mechanism:
1. reduced BF to kidney 2. adrenal cortex stim by the renin-angiotensin feedback 3. aldosterone released 4. renal tubule level: Na retention, K excretion |
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desoxycorticosterone pivilate (DOCP)
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desoxycorticosterone pivilate (DOCP)= percorten V
- pivilate: long acting - synthetic mineralocorticoid - addison's: hypoadrenocorticism (gluco and mineralo), add low dose pred for additional glucocorticoid supplement - irritation at inj site: deep IM in carnivores - lasts 25 days |
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mineralocorticoid modifications
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mineralocorticoids:
1. 21 hydroxyl groups essential 2. 9 fluorination enhances activity, along with glucocorticoid activity (fludrocortisone Florinef RX) 3. substitution on C16 D ring elimate mineralocorticoid activity: dex and betamethasone |
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mineralocorticoid actions
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mineralocorticoid action:
- renal distal tubule: increases Na absorption - enhance K and H excretion - require functioning kidney to be effective |
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Glucorticoids: gen
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glucorticoids:
- endogenous hormone - physiological dose: replaces deficient - derived from adrenal cortex - |
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glucocorticoids: use
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glucorticoids use:
1. anti-inflammatory 2. immunsupressive effects - not selective: can cause side effects |
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glucorticoids: mechanism
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glucocorticoids mechanism:
1. pass through mem of cells within target tissue 2. bind intracytoplasmic steroid receptors 3. steroid-receptor complex passes to nucleus and associates with DNA to alter gene transcription 4. controls cellular processes - stabilizes cell mem: use in shock patients |
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glucocorticoids: chemistry
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glucorticoids:
- block phospholipase A2 in prostaglandin synthesis: blocks arachadonic acid, lipoxygenase and COX 1 and 2 - leading to prostaglandin, thromboxane and leukotrienes - also neutrophil migration into tissues |
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glucocorticoids: metabolic effects
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glucorticoids metabolic effects:
1. raise blood glc: gluconeogenesis enhanced in extrahepatic tissue, insulin antagonism increase hepatic glycogen storage 2. increased protein catabolism= increased protein levels in liver and plasma= muscle atrophy 3. lipolysis: mobilization of fa's and redistribution of fat from peripheral to central 4. reduces intestinal absorption 5. increases excretion of Ca |
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glucocorticoids: physiological effects
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1. antagonizes release/ or effect of ADH: conserve H2O
2. reduced intestinal absorption: dec abs PO drugs 3. enhanced secretion of gastric acid, pepsin, trypsin: chronic use antiacid (carafate, ranitidine) to prevent ulcers 4. reduced production and altered nature of gastric mucus 5. cutaneous atrophy 6. increased mobilization of Ca: osteoporosis |
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glucocorticoids: hemodynamic effects
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glucocorticoids antagonist to:
1. fibrin deposition 2. fibroblast proliferation and formation of collagen: reduces scar tissue 3. platelet aggregation 4. capillary BF and vasodilation: causes edema formation/ loss of protein and leukocytes from vasculature into inflammed tissue |
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glucocorticoids: inflammatory effects
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glucocorticoids:
1. supress inflammatory fx of leukocytes by stabilizing cell membranes: granulocytes, mast cells, monocytes/macro 2. prevent release of histamine and arachadonic acid metabolites of cyclooxygenase and lipoxygenase pathways |
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glucocorticoids: immune applications
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glucocorticoids:
1. immunosupression in cutaneous hypersensitivity disease 2. immune mediated or autoimmune disease, eg IMHA 3. thrombocytopenia 4. immune-mediated polyarthritis: chose over NSAID |
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corticoid modifications
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- corticosteroids are hormones secreted by the adrenal cortex or synthetic analogs
- modification of the naturally occuring glucocorticoid nucleus causes changes in characteristics - only difference between hydrocortisone and prednisolone is a double bond |
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glucocorticoid: modifications
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glucorticoids:
1. 6 fluorination 2. 9 fluorination 3. 16 OH 4. 16 CH3 - prednisolone derivatives - all contraindicated in pregnant animals: miscarriage or tertaology |
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16 CH3 glucocorticoids
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16 CH3 glucocorticoids:
reduces Na retaining potency |
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16 OH glucocorticoids
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16 OH glucocorticoids:
- reduces mineralo and gluco activity - good in not very sick animals or don't want Na retention |
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9 fluorination glucocorticoids
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9 fluorination glucocorticoids:
- enhances gluco and mineralo activity - use in hypoadrenocorticism |
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6 fluorination glucocorticoids
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6 fluorination glucocorticoids:
- enhances activity without enhancing mineralo- activity - good in cardiac P |
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cortisone and hydrocortisone
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- both small anti-inflammatory and salt retaining
1. hydrocortisone:HL 120min, use topically 2. cortisone: HL 30min, precursor metabolized in liver to hydrocortisone |
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prednisone and prednisolone
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- anti-inflammatory 4, small salt retaining
1. prednisone: HL 60min, increases urination 2. prednisolone: HL 116-212 min, cellular level, use in dermatology bc often metabolic dz |
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6 alpha methyl prednisolone and triamcinolone
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- anti-inflammatory 4-5, no salt retaining
1. 6 alpha methyl prednisolone: HL 78-188 min 2. triamcinolone: HL 200+ min, once weekly, increase Na retention in horse |
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dexamethasone and betamethasone
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- anti-inflammatory 30-35, no salt retention
- methylated: penetrates because more lipophilic 1. dexamethasone: HL 100-210min, increased Na retention in horse 2. betamethasone: HL 300+ min |
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aldosterone, 11-deoxycorticosterone and fludrocortisone
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1. aldosterone: small anti-inf, salt retaining 800, HL 80 min
2. 11-deoxycorticosterone: no anti-infl, salt retaining 40, HL 60min 3. fludrocortisone (fluorinef): anti-infl 10, salt retaining 800, HL 300+ min |
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glucocorticoid: anti-inflammatory mechanism
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glucorticoid:
1. stabilizes leukocytes lipsomal enz 2. prevents release of destructive acid hydrolase 3. inhibits macrophage accumulation in inflammed 4. reduced leukocyte adhesion to capillary endothelium 5. reduces capillary wall permeability and edema formulation 6. decrease compliment components 7. antagonizes histamine activity and release of kinin from substrates 8. reduces fibroblast proliferation, collagen deposition, and subsequent scar formation |
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glucocorticoid: immune supression mechanism
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glucocorticoid
1. reduces activity and volume of lymphatic system 2. produces lymphocytopenia 3. decreases Ig and complement concentration 4. decreases passage of immune complexes through basement membranes 5. possibly depresses reactivity of tissue to antigen-Ab interactions |
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glucocorticoids: indications
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glucocorticoids:
- use in stressed or shock - therapeutic index high: can give high dose if not given continuously |
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glucorticoids: immunosupression
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glucorticoids immunosupression:
1. mast cells decreased in numbers, histamine depressed 2. decreased circulating T lymphocytes 3. reduces production of inteferon |
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glucorticoids: adverse effects
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glucorticoids:
1. adrenal atrophy reversible after stop, but can have hypoadrenocorticism if withdraw suddenly 2. excessive gluconeogenic, hepatomegaly 3. hyperglycemia: signs PU, PD, weight gain - cats: caused by stress - dogs: PU/PD especially 4. long term admin produces proteinuria 5. thin, alopecia skin in chronic |
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glucorticoids: potential ADR
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glucorticoids potential ADR:
1. hypertension 2. Na and H20 retention 3. gastric ulceration 4. osteoporosis: more in humans |
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glucocorticoids: blood
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glucocorticoids:
1. stimulate erythroid cells of bone marrow 2. prolong survival time of RBCs and platelets 3. neutrophila, eosinophilia |
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glucocorticoids: products
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glucocorticoids:
1: methylated: beclomethasone and betamethasone 2. cortisone 3. dexamethasone 4. flunisolide: no adrenal fx 5. hydrocortisone 6. me(thyl)prednisone: use in COPD, cong heart failure b/c low Na retention and good anti-inflammatory 7. methylprednisolone 8. paramethasone 9. prednisone, prednisolone 10. triamcinolone: problems in horse 11. fludrocortisone: very potent mineralo prop |
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glucocorticoids: potencies
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glucocorticoid potencies:
1. flumethasone 2. betamethasone 3. dexamethasone: use in cattle b/c 0 withdrawl date 4. fluoroprednisolone 5. triamcinolone 6. methylprednisolone 7. prednisone 8. prednisolone 9. cortisone 10. hydrocortisone |
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Equipose- Boldenone
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Equipose- Boldenone:
- anabolic steroid - approved in horses, but not stallions and pregnant due to lack of data - illegal in professional horses - reverses tissue depleting processes and restores constructive metabolism - adjunct with other therapy and high protein diet |
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stanazolol
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stanazolol: anabolic steroid
- controlled, availability problems - stim of erythropoeisis process - dog, horse - long acting, very lipophilic |
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nandrolone (durabolin)
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nandrolone (durabolin):
- anabolic steroid - human product used in small animals for refractory anemia - now use EPO as replacement |
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prednisone/ prednisolone
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prednisone/ prednisolone:
- used for several weeks or months to get chronic processes under control - when under control: taper to EOD or adrenals will atrophy/ without it animal cannot respond to stress= circulatory crisis - hypoglycemia, depression |
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corticosteroids: eye
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corticosteroids: eye:
- can cause systemic side effects - corneal and anterior uveal dz: 1% pred acetate and 0.1% dex - most systemic steroids penetrate blood-aqueous barrier, used to treat intraocular inflammation |
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corticosteroids: eye effects
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corticosteroids eye effects:
1. decrease cellular infiltration 2. inhibits fibroblastic and collagen-forming activity 3. diminishes neovascularization 4. stabilizes lysosomes 5. can cause increased intraocular pressure and possibly cataracts in cats |
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glucocorticoids: main points
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glucocorticoids: main points:
1. can cause miscarriage 2. never use with NSAIDs: blockage of good prostaglandins 3. spinal trauma use solumedrol then switch to NSAID 4. contraindicated in head trauma |
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glucorticoids: withdrawl symptoms
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glucorticoids: withdrawl symptoms:
1. dullness, depression 2. decreased exercise tolerance 3. incoordination 4. weight loss 5. lose stools 6. behavior changes |
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glucocorticoids: diabetes
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glucocorticoids: diabetes:
- steroid- associated insulin resistance can make pre-exisitng diabetes much harder to treat - can tip stable diabetics into crisis - even topical absorption can have an effect on diabetic control |
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glucocorticoids: shock
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glucocorticoids: shock:
- high dose controversial in hypovolemic shock tx - inhibits the arachadonic acid casade: 1. decreases cellular inflammation -but- 2. can result in gastric ulceration and bleeding via inhibition of COX 1 formation 3. hypoxic induced GI mucosa may be further damaged by therapy, even after 1 or 2 doses |
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glucocorticoids: contraindications
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glucocorticoids: contraindications:
1. infectious dz 2. diabetes mellitus 3. liver dz 4. protein-losing nephropathy 5. pregnancy 6. immature animals: inhibits growth 7. wound or fracture healing: if use, must give antibiotic 8. corneal ulceration/ infection: risk of corneal perforation, delayed repair, secondary infection |
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glucocorticoids: indications
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glucocorticoids: indications:
1. documented shock from Addisonian crisis 2. asthma attacks 3. bad itchy skin 4. IBD 5. chronic active hepatitis 6. lymphoma 7. uveitis |
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glucocorticoids: adverse effects
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glucocorticoids: adverse effects:
1. metabolic: diabetes mellitus, hyperlipidemia, hepatopathy 2. musculoskeletal: atrophy, ligament weakness 3. immun: increased risk of inf and septicemia 4. endocrine: hypothalamo/ pituitary axis, thyroid and parathyroid supression 5. GI: ulcers, pancreatitis 6. fluid balance: water retention, PU/PD 7. anaphylatic rxns 8. abortion: use dex to get dairy cows to calve |
