Drugs for hormone and Metabolic disorders

Trilostane

By M. Younus, BVSc, MVSc, SKUAST-K

Trilostane(epoxy steroid).

  • Approved for Dogs in chusing syndrome.

MOA:

  • Trilostane is a steroidogenesis inhibitor and inhibits the production of all classes of steroid hormones, including androgens, estrogens, progestogens, glucocorticoids, and mineralocorticoids.

Effects:

  • Inhibiting  the production of corticosteroids such as cortisol and aldosterone in the adrenal glands.
  • Abortifacient due to its inhibition of progesterone synthesis

Side effects:

  • Lethargy.
  • Vomiting and diarrhea.
  •  Lack of appetite during the first few days of therapy.

Dose:

  • 2.2 to 6.7 mg/kg PO O D and start with the lowest possible dose based on body weight.
  • Use Dexamethasone at a dosage of 0.15 mg/kg PO,  in a possible addisonian crisis. 

Species:

  • Dogs

Indication:

  • Pituitary-dependent hyperadrenocorticism (PDH).
  • Adrenal-dependent hyperadrenocorticism (ADH).

Contraindication:

  • Hypersensitivity. 
  •  Pregnant animals.

Brands:

  • Vetoryl 30mg Cap ( Dechra Ltd)(offered by GNH India).

Comoposition:

Each cap contains 30mg Trilostane.

Propylene glycol (PG)

By M. Younus, BVSc, MVSc, SKUAST-K

Propylene glycol (1,2-propanediol).

  • Sweet, hygroscopic, viscous liquid.
  • Gluconeogenic drug for prevention and treatment of ketosis in lactating cows.

MOA:

  •   Major quantity  of PG is absorbed  from the rumen  wall or gastrointestinal tract and is converted to glucose by the liver.
  •  Some quantity of PG  in the rumen is converted to  propionate and propanal. Propanal is converted to propanol, which in turn is  converted to propionate.  propionate is converted to glucose in the liver.   
  •  PG is also  metabolized to lactate, acetate, and pyruvate in the liver.  Lactate enters gluconeogenesis via pyruvate, which can be converted to  oxaloacetate.   When the oxaloacetate is sufficient for citrate synthase to combine  with acetyl-CoA, the excessive acetyl-CoA is utilised for formation of citrate .   

Effects:

  •   Increase in blood glucose level and decrease fat percentage of milk.  
  • Maintenance of positive energy balance.
  • The anti-ketogenic properties of PG are partly due to prevent acetyl-CoA conversion to ketone bodies (β-hydroxybutyrate, acetone, and acetoacetate) and  increasing the  oxidation of acetyl-CoA into the TCA-cycle and the supply of  gluconeogenic glucose.  

Therefore  feeding Propylene glycol  can  attribute to an increase in feed intake and subsequent supply of more glucogenic substrate.

Side effects:

  •  Depression, ataxia, and excessive salivation as well as abnormal, malodorous, and foul breath. 

Drug combination:

  Butaphosphan-cyanocobalamin  , glucocorticoids , L-carnitine-methionine , and glucose with PG  are beneficial in improving the  chances of the resolution of ketosis compared to PG when used alone. 

Species:

  • Cattle.

Dose:  

Treatment of ketosis. 

  • 300 g of PG daily to ketonic animals 3-5days. The maximum feeding level of PG is 500 g per day. 

Prevention of  ketosis.

300 g of PG daily  one week prior to parturition.

Indications:

  •  Treatment and prevention  of ketosis.
  •  Increase feed consumption.
  • To increase reproductive performance.
  • To increase milk production.

Contra indication: 

  •  Do not feed more than 500 g PG daily.
  • Cats 

Brands:

  • Dynapro vet 600ml liquid (Epicon India).

Composition:

Propylene Glycol, Glycerol, Calcium Propionate, VFA, Chromium, Niacinamide.

  • Vety -boost 1liter liquid( Vetcare BSA pharma India).

 Composition: 

Propylene Glycol Nicotinamide Sodium Acid Phosphate Gluconeogenic Phytochemical additives .

  • Ketoscare 1lter liquid( Zenley Animal Health India).

 Composition: 

Propylene Glycol, Niacinamide, Sodium Acid Phosphate & Gluconeogenic Phytochemical Additives.  Gluconeogenic precursors fortified with B-Complex’s, Vitamins & Minerals    

Glycerol

By M. Younus, BVSc, MVSc, SKUAST-K

Glycerol (biodiesel by product)

  •  Belongs to alcohol family.
  •   Structural component of triglycerides and phospholipids.
  •  Glycogenic and anti-ketogenic agent. 
  •  Estimated caloric value of glycerol  ranges from 1.98 to 2.26 Mcal NEL/kg.

MOA:

  • Glycerol in the rumen is fermented into propionate and butyrate, at the expense of acetate.
  • The decrease of acetate leads to low fat production in Milk.
  • The liver converts propionate into glucose and starch.
  • Glycerol also lowers levels of blood non-esterified fatty acids (NEFA) and beta-hydroxybutyric acid (BHBA).

Effects:

  •   Increase in blood glucose level and decrease fat percentage of milk.  
  • Maintenance of positive energy balance.

Therefore  feeding glycerol can  attribute to an increase in feed intake and subsequent supply of more glucogenic substrate.

Other properties of Glycerol:

  • Acts as antimicrobial agent.
  • Being hygroscopic act as laxative.
  • Retain water in the body system.

Species:

  • Cow ,Dog and Horse

Side effects:

  • Diarrhoea,  vomiting and  excessive bowel activity

Dose:

  • 240ml / Cow PO OD X 10days.
  • 30mL to 60mL PO OD in Horse.

Indications:

  •  Treatment of ketosis.
  •  To increase feed consumption.
  •  As prophylactic to maintain energy balance in transient cow.
  •  To increase breathing and digestion in horse.
  •  As topical application for wound healing.
  •  As moisture agent in dry skin condition.
  •  As  rectal pessary for softening of stools in dog.
  •  As emergency treatment for glaucoma in dog.

Contra indication: 

  •  Lactating  and Pregnant Mare.
  •  Horse having abdominal discomfort.
  •   Severe Diarrhoea

Brands:

  •  Oral Glycerol 100ml( Medi plus India).
  • Glycerine 6OOg food grade( Puramio )
  •   G-Sol Glycerine 500 g Oral Solution(Eleesa India).

Calcium

By M. Younus, BVSc, MVSc, SKUAST-K

Calcium ( In organic element).

  • Essential Metabolic elements.
  • Important for milk production.
  • Important for bone growth.
  • Important for nerve transmission.
  • Important for muscle tone.

MOA:

  • Calcium (Ca2+) acts as a second messenger, in neurotransmitter release from neurons. It causes contraction of all muscle cell types, and fertilization.  
  •  Ca ions maintain the potential difference across excitable cell membranes.

Effects:

  • Contractions of SK muscles, Smooth muscles and Cardiac muscles.
  • Transduction of nerve impulses.

Side effects:

  • Cardiotoxicity.
  • Impairment of appetite.
  • Muscles tremors.
  • Constipation and bloat.

Drug combination:

  • Ca + P+ Mg + Dextrose is used to treat four disease at a time

Species:

  • Cattle.
  • Sheep and  Goat. 
  • Mare.
  • Bitch.

Dose:

  • Bitch
    20 ml calcium of  1.86% W/V– IV.
  • Sheep and  Goat
    50-150ml  of 1.86% W/V calcium  IV.
  • Cattle
    Upto 800 ml of 1.86% W/V calcium  IV.
    40- 80 g ionic Calcium P O.

Indication:

  • Parturient paresis/ milk fever in ruminants.
  • Eclampsia in bitch and mare.

Contraindication:

  • Cardiac distress.
  • Rapid adminstration .
  •  Don’t use  unused solution second time.

Brands:

  • Calcium boro gluconate 450 ml Inj bottle( Vetquinol India).

Composition: 1.86% W/V Calcium.

  • Borocal 450 ml Inj bottle( Vetindia India).

Composition: 1.86% W/V Calcium.

  • Mifex 450 ml inj bottle ( Elanco India).

Composition:
1.86% W/V Calcium.
5% W/V Magnisium hypophosphite.
20% W/V Dextrose.

  • Milk fever 450 ml inj plastic bottle( Zydus India).

Composition:
1.86% W/V Calcium.
5% W/V Magnisium hypophosphite.
20% W/V Dextrose.

  • Calup 300ml  gel tube ( Vet Care India).

Composition:  Each tube contains 43.5 g ionic Calcium.

  • Calcimust 300 ml gel tube ( Vet Mankind India).

Composition: 

Each tube contains:

  1. 6600mg calcium. 
  2. 3400mg  Phosphorus.
  3.  32,000 IU Vit D3.   
  4. 400mcg Vit B12.
  5.  200mg  /100gm Pueraria Mirifica extract. 
  • Recal 300ml gel tube( Rift Animal Care India).

Composition:
Each 10 gm  Contains:

  1. 660mg Calcium(ca ++). 
  2. 330mg  Phosphorus.                              
  3. 38000i.u. Vitamin D3.   
  4. 400mcg Vitamin B12. 
  5. 125mg  Cobalt.
  6. 30mg  Manganese. 
  7.  250mg  Zinc. 
  8. 1000mg  Propylene glycol. 
  9. 10000mg Carbohydrate.                        

Sodium Acid phosphate(SAP)

By M. Younus, BVSc, MVSc, SKUAST-K

Sodium Acid phosphate (Sodium dihydrogen phosphate or Mono sodium phosphate).

  • Phosphate is an essential electrolyte and  important constituent of cell membranes, DNA/RNA, ATP and intracellular signaling proteins.

MOA:

  • Sodium acid phosphate in body  dissociates into sodium ion  and phosphate ion. Phosphate ion has following actions.
  • Combines with Ca to form hydroxyapatite.
  • Stimulates PTH secretion.
  • Stimulates fibroblast growth factor 23.
  • It  also carries out oxidative phosphorylation.
  • Sodium phosphate when taken orally increases the amount of solute present in intestine thus creating an osmotic gradient. 

Effects:

  • Skeleton growth and development.
  • Metabolic effect ( carbohydrate/ fat / protein metabolism) . 
  •  Growth, maintenance, and repair of cells and tissues.
  •  laxative effect.
  • Production of  ATP.
  • Muscle contractions.
  • Normal heartbeat.
  • Nerve signaling.

Side effects:

  • Hyperphosphatemia cause muscle cramps, tetany, Diarrhoea, Cardio vascular problems, perioral numbness, and tingling.

Species:

  • Many species.

Dose:

Special dose: Postparturient hemoglobinuria in cattle.

  • 60g in 300ml distilled water IV followed by S/ C same dose at 12 hour interval.
  • 60g PO for cattle till disappearance of acute symptoms.
  • 30 g PO as prophylaxis in aged and senile Dairy cattle.

General dose( In other  conditions):

  • 5-10 ml(providing phosphorus  8% w/v) IM/ IV/ SC twice a week in cattle & horses 
  •   1-3 ml( providing phosphorus 8% w/v) IM/ IV/ SC twice a week in small animals.

Indication:

  • Post Parturient hemoglobinuria in cattle.
  • General debilitating diseases.
  • Infertility.
  • Low Milk production.
  • Ketosis.
  • Indigestion in horses and other animals.
  •  Treatment of hypercalcaemia.
  • Treatment of constipation. 

Contraindication:

  • Renal disease( CKD).
  • Cardiovascular calcinosis.
  •  Hypernatremia.

Brands:

  • Sodaphos 100g powder( Zydus Animal Health India).

Composition:99% w/w Sodium acid phosphate.

  • Vetphos 100g powder( Geevet India).

Composition: 99% w/w Sodium acid phosphate.

  • Power- Phos 400g powder ( Allied Chemicals India).

Composition: 99% w/w Sodium acid phosphate.

  • Protiphos 500g granules( Healthy vet India).

Composition: 99% w/w Sodium acid phosphate.

  • Urimin 30ml/100ml inj vial( Verbac India).
    Composition:     Each ml contains 40.3% w/v Sodium Acid Phosphate.                  
  • Hi-Fos 30ml inj vial ( Zenley Animal Health India).

Composition: Each ml contains 40.3% w/v. Sodium Acid Phosphate. 

  • Vet-Phos 30ml inj vial ( Geevet India).

Composition: Each ml contains 40.3% w/v Sodium Acid phosphate.

  • M-Phos 30ml inj vial ( Hi-tech India)

Composition: Each ml contains 400mg Sodium Acid phosphate and100 mcg Methyl cobalamin. 

  • Nicophos-M 30ml/100ml inj vial ( Nicosia India).

Composition: Each ml contains 400mg Sodium Acid phosphate and100 mcg Methyl cobalamin.

Bexagliflozin

By M. Younus, BVSc, MVSc, SKUAST-K

Bexagliflozin ( hypoglycemic drug).

  • Anti diabetic medicine for cats. 
  • Approved by the FDA.

MOA:

  • Bexagliflozin is sodium-glucose cotransporter 2 (SGLT2) inhibitor. 
  • Prevents the cat’s kidneys from reabsorbing glucose into the blood.
  • Causing excess glucose to be passed out in the urine.

Effects:

Drop in blood glucose level.

Side effects:

  •  Diabetic ketoacidosis or euglycemic diabetic ketoacidosis, both of which may result in death. 

Species:

  • Cats. 

Dose :

  •  5mg/kg PO OD via a flavored tablet. 

Indication:

  •   Diabetes mellitus not previously treated with insulin.

Contraindication:

  •  Dehydration.
  • Anorexia.
  • Cats on insulin.
  • Ketoacidosis.

Brands:

  •  Bexacat 15mg tab ( Elanco USA).

Composition: Each tab contains 15mg Bexagliflozin.

Ertugliflozin

By M. Younus, BVSc, MVSc, SKUAST-K

Ertugliflozin  ( hypoglycemic drug).

  • Anti diabetic medicine for horses. 
  •  Extra label use.

MOA:

  •  Ertugliflozin   is sodium-glucose cotransporter 2 (SGLT2) inhibitor. 
  • Prevents the horse’s kidneys from reabsorbing glucose into the blood
  • Causing excess glucose to be passed out in the urine.

Effects:

  • Lower blood glucose.
  • Returns insulin to normal or near-normal levels.
  • Reduce fats deposits.

Side effects:

  • Weight loss
  • Urinary tract infection.
  • Excessive urination.
  • Excessive drinking. 
  • Risk of renal failure.
  • Hypertriglyceridemia.

Species:

  •  Horse

Dose :

  •   0.05 mg/kg once daily, for at least 30 days. 

indication:

  •   Equine Metabolic Syndrome.

Contraindication:

  •  Dehydration.
  • kidney disease.
  •  Use cautiously when horse is on NSAIDS.

Brands:

Available as human brands in India.

  •  Steglatro 15mg tab ( MSD India).

Composition: Each tab contains 15mg Ertugliflozin .

Levothyroxine

By M. Younus, BVSc, MVSc, SKUAST-K

Levothyroxine (synthetic levoisomer of thyroxine (T4)).

  • Approved for hypothyroidism in dogs.
  • Extra label use for cats.

MOA:

  • Levothyroxine in body  is converted into active metabolite
    triiodothyronine (T3) in the peripheral tissues.
  •  T3 enters into nucleus of the cell where it forms complex with the receptors. 
  • This receptor complex  is responsible for protein synthesis. 
  • The proteins produced are required in the regulation of  different cellular functions.
  • T4 and T3 also possess cardiac stimulatory effect.

Effects:

  • Growth and development.
  • Metabolism of proteins,carbohydrates and lipids.
  • Maintaining the heart rate, skin moisture, gut motility, thermoregulation, normal weight and memory.

Side effects:

  • Decreased appetite.
  • Vomiting and diarrhoea.
  • Itching.
  • Hyperactivity.
  • Polyurea.

Species: 

  • Dog, Cat and Horse.

Dose:

  • 20 μg/kg PO BD in dog.
  •  10-20 μg/kg PO OD in cat.
  •   0.1 mg/kg PO OD 3-6 months, that is  48 mg/day   in horses weighing 450 to 525 kg and 24 mg/day in small horses and ponies 

Indication: 

  • Hypothyroidism in dog and cat.
  • Equine Metabolic Syndrome.

Contraindication:

  • Levothyroxine should not be given without diagnosis of hypothyroidism.
  • Allergy to Levothyroxine.

Brands:

  • Thyro-Tab canine ( Lloyd Inc USA- Exported by GNH India ).

Composition: Each tab contains 0.7mg Levothyroxine.
Human brands in India.

  • Thyronorm 120 tab bottle( Abbot India).

Composition: Each tab contains 25cmg/ 50mcg/ 75 mcg Levothyroxine.

  • Eltroxin 60 tab bottle( Glaxo Smith India).

Composition: Each tab contains 25mcg/ 50mcg/ 75 mcg Levothyroxine

  •  Lethyrox 100 tab ( Intas India).

Composition: Each tab contains 25mcg/ 50mcg/ 75mcg Levothyroxine.

Pergolide

By M. Younus, BVSc, MVSc, SKUAST-K

Pergolide (Ergot derivative)

  • Approved for Pituitary pars intermedia dysfunction PPID in horse 

MOA:

  •  Pergolide  acts on the dopamine D2 and D3, alpha- 1and alpha2- adrenergic, and 5-hydroxytryptamine (5-HT) receptors.It acts as agonist on these receptors and modelates the production of dopamine.

Effects:

  • Reduction in excessive production of protein hormones and other mediators.

Side effects:

  •  Decrease in appetite.
  •  Diarrhea, and colic.

Species:

  • Horse

Drug combinations:

  •  Cyproheptadine (0.25 mg/kg PO SID), a serotonin antagonist, has been combined  with pergolide   with some success. 

Dose:

  • 0.2–5.0 mg PO  OD life time.
  • Most horses show improvement with doses of 0.75 to 1.5 mg/d of pergolide.
  •  Improvement is evident by 6 weeks of treatment and includes shedding of the hair coat, a decrease in plasma ACTH concentration, and a decrease in glucose concentration.

Indication:

  • Pituitary pars intermedia dysfunction (PPID)/Equine Cushing’s disease.

Contraindication:

  • Do not administer with MAOIs.

Brands:

  • Prascend tab ( Boehringer Ingelheim USA).

Composition: Each tab contains 1mg pergolide.

Selegiline

By M. Younus, BVSc, MVSc, SKUAST-K

Selegiline (L-Deprenyl ).

  •  FDA-approved for use in dogs. 
  •  Off label drug for use in cats.
  •  For the treatment of canine cognitive dysfunction and pituitary-dependent Cushing’s disease.

MOA: 

  • Selegiline , selectively and reversibly inhibits,  monamine oxidase-B (MAO-B).
    MA O-B  plays role in catabolism of dopamine and catecholamines.
  •  L-desmethylselegiline, amphetamine, and methamphetamine are the metabolites of selegiline.  
  • These metabolites act as CNS stimulants. 

Effects:

  • Rise in dopamine levels in the brain leads to control of pituitary dependent of hyperadrenocorticism.
  • Rise in level of catecholamines in the brain leads to increase in cognitive function.

Side effects:

  • GIT upset.
  • Nervous signs like restlessness, hyperactivity, repetitive, and salivation.

Species:

  • Dog and Cat.

Dose:

  • 0.5-1.0 mg /kg PO for treatment of cognitive dysfunction.
  • 1.0-2mg / kg PO for treatment of cushing disease.
    Start with lower dose.

Indication:

  • Cognitive dysfunction
  • Pituitary dependent hyperadrenocorticism. 

Contraindication:

  • Hypersensitivity reactions.
  • Dogs showing agression.
  • Concurrent use of opioids.

Brands :

  • Anipryl 5mg / 10mg/15mg/30mg tab ( Zoetis USA).

Composition: Each tab contains :5mg selegiline/ 10mg selegiline/15mg selegiline/30mg selegiline.
Human brands in India: 

  • Eldepryl 5mg / 10mg tab( Themis Medicare India).

Composition: Each tab contains 5mg selegiline/ 10mg selegiline.

  • Elegiline 5mg tab( Sun India).

Composition: Each tab contains 5mg selegiline.

  • Jumax 5mg tab( Torrent India).

Composition: Each tab contains 5mg selegiline.

  • Jumix 5mg tab( Sanofi Aventis  India).

Composition: Each tab contains 5mg selegiline.

  • Selerin 5mg tab( Cipla India).

Composition: Each tab contains 5mg selegiline.

  • Selgin 5mg tab( Intas India).

Composition: Each tab contains 5mg selegiline.

 

Methimizole

By M. Younus, BVSc, MVSc, SKUAST-K

Methimizole and Carbimazole  (Antithyroid agents).

  • Carbimizole is pro drug of Methimizole.
  • Methimizole is also known as Thiamazole.
  • Methimazole is a thioamide inhibitor of the enzyme thyroid peroxidase (TPO).

MOA:

  •  These drugs  decrease the uptake and concentration of inorganic iodine by thyroid, and also reduce the formation of di-iodotyrosine and thyroxine. 
  • Carbimazole  is converted to its active form of methimazole
  • Methimizole prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, so reducing the production of the thyroid hormones T3 and T4.

Effects:

  • Decrease secretion of Thyroid hormones.

Side-effects:

  • Vomiting, anorexia, and tiredness. and usually occur within the first three months of treatment. 
  • Mild changes in  blood cell counts are usually temporary and resolve with time.

dose:

  • Start with 5–15 mg/day divided twice daily.
  • After 2–3 weeks of treatment perform serum T4, CBC, platelet count, and serum chemistry profile. The dose of methimazole is adjusted according to serum T4 levels.
  • Repeat levels  every 2–3 weeks until serum T4 concentrations are in the normal range. 
  • Discontinue treatment if agranulocytosis, thrombocytopenia, anemia, or azotemia occur. 

species:

  • Cat and Dog.

Indication:

  • Hyperthyroidism in cat and dog.

Contraindication:

  • Hypersensitivity to Methimizole and Carbimazole.
  • Low platelet count.
  •  Liver failure.

Brands:

Human brands in India.

  • Methimez 5mg/ 10mg Methimizole tablet ( Sun India).
  • Metnimez5mg/ 10mg Methimizole tablet ( Sun India). 
  • Neo-mercazole 5mg/10mg Carbimazole tablet( Nicholas India).
  • Thyrocarb 5mg/10mg Carbimazole tablet (Abbot India).
  • Thyrozole 5mg Carbimazole tablet ( Cadila India).