Target species
Horses (non-food producing)
Indications for use
Symptomatic treatment of clinical signs associated with Pituitary Pars Intermedia Dysfunction (PPID) (Equine Cushing's Disease).
Contraindications
Do not use in horses with known hypersensitivity to pergolide mesilate or other ergot derivatives or to any of the excipients.
Do not use in horses less than 2 years of age.
Special warnings
Appropriate endocrinologic laboratory tests should be conducted as well as evaluation of clinical signs in order to establish a diagnosis of PPID.
Special warnings for use in the target species
As the majority of cases of PPID are diagnosed in aged horses, other pathological processes are frequently present. For monitoring and frequency of testing, see Amounts to be administered and administration route.
Special precautions to be taken by the person administering the veterinary medicinal product to animals
This product may cause hypersensitivity (allergy) reactions. People with known hypersensitivity to pergolide or other ergot derivatives should avoid contact with the veterinary medicinal product.
This product may cause adverse effects due to decreased prolactin levels, which poses a particular risk to pregnant and lactating women. Pregnant or lactating women should avoid dermal contact or hand-to-mouth contact and wear gloves when administering the product.
Accidental ingestion, especially by children, may cause adverse reactions such as emesis, dizziness, lethargy or low blood pressure. To avoid accidental ingestion, the blister should be replaced into the carton and carefully kept away from children. Avoid hand-to-mouth contact. Do not eat, drink or smoke when using this product. In case of accidental ingestion, seek medical advice immediately and show the package leaflet or the label to the physician.
This product may cause eye irritation. Avoid contact with the eyes including hand-to-eye contact when handling the tablets. Minimize exposure risks when dissolving the tablets, e.g. tablets should not be crushed. In case of contact of the dissolved product with skin, wash exposed skin with water. In the event of eye exposure, flush the affected eye immediately with water and seek medical advice.
Wash hands after use.
Adverse reactions
Horses:
Rare (1 to 10 animals / 10,000 animals treated):
Inappetence, anorexia1, lethargy1. Central nervous system signs2 (e.g. depression2, ataxia2) . Diarrhoea, colic.
Very rare (<1 animal / 10,000 animals treated, including isolated reports):
Sweating.
1 transient
2 mild
Reporting adverse events is important. It allows continuous safety monitoring of a veterinary medicinal product. Reports should be sent, preferably via a veterinarian, to either the marketing authorisation holder or its local representative or the national competent authority via the national reporting system. See also section ‘contact details' of the package leaflet for respective contact details.
Use during pregnancy and lactation
Pregnancy: Use only according to the benefit/ risk assessment by the responsible veterinarian. The safety of this veterinary medicinal product has not been demonstrated in pregnant mares. Laboratory studies in mice and rabbits have not produced any evidence of teratogenic effects. Reduced fertility was seen in mice at a dose of 5.6 mg/kg body weight per day.
Lactation: The use is not recommended in lactating horses, in which the safety of this veterinary medicinal product has not been demonstrated. In mice, reduced body weights and survival rates in the progeny were attributed to the pharmacological inhibition of prolactin secretion resulting in lactation failure.
Interactions
Use with caution in case the veterinary medicinal product is co-administered with other drugs known to affect protein binding.
Do not administer concurrently with dopamine antagonists, such as neuroleptics (phenothiazines - e.g. acepromazine), domperidone, or metoclopramide, as these agents may reduce the effectiveness of pergolide.
Amounts to be administered and administration route
Oral use, once daily.
To facilitate administration, the required daily dose should be placed in a small amount of water and/or mixed with molasses or other sweetener and agitated until dissolved. In this case, the dissolved tablets should be administered with a syringe.
The whole amount should be administered immediately. Tablets should not be crushed, see Special precautions to be taken by the person administering the veterinary medicinal product to animals.
Starting dose:
The starting dose is about 2 µg pergolide/kg (dose range: 1.3-2.5 µg/kg; see table below). The maintenance dose should then be titrated according to the individual response as determined by monitoring (see below), resulting in an average maintenance dose of 2 µg pergolide/kg body weight with a dose range of 0.6-10 µg pergolide/kg body weight.
Starting doses are recommended as follows:
Horse body weight
0.5 mg tablet
1 mg tablet
2 mg tablet
Starting dose
Dosage range
200-400 kg
O
0.5 mg
1.3-2.5 µg/kg
401-600 kg
O
1.0 mg
1.7-2.5 µg/kg
OR
401-600 kg
OO
1.0 mg
1.7-2.5 µg/kg
601-850 kg
O
+
O
1.5 mg
1.8-2.5 µg/kg
OR
601-850 kg
OOO
1.5 mg
1.8-2.5 µg/kg
851-1000 kg
O
2.0 mg
2.0-2.4 µg/kg
OR
851-1000 kg
OO
2.0 mg
2.0-2.4 µg/kg
Maintenance dose:
Lifelong treatment is anticipated for this disease.
Most horses respond to therapy and are stabilised at an average dose of 2 µg pergolide/kg body weight. Clinical improvement with pergolide is expected within 6-12 weeks. Horses may respond clinically at lower or varying doses; it is therefore recommended to titrate to the lowest effective dose per individual based on response to therapy, whether it is effectiveness or signs of intolerance. Some horses may require doses as high as 10 µg pergolide/kg body weight per day. In these rare situations, appropriate additional monitoring is advised.
Following initial diagnosis, repeat endocrinologic testing for dose titration and monitoring of treatment at intervals of 4-6 weeks until stabilisation or improvement of clinical signs and/or diagnostic testing occurs.
If clinical signs or diagnostic testing have not yet improved at the first 4-6 week interval, the total daily dose may be increased by 0.50 mg. In case clinical signs have improved but are not yet normalised, the veterinarian may decide to titrate or not to titrate the dose, considering the individual's response/tolerance to the dose.
In case clinical signs are not adequately controlled (clinical evaluation and/or diagnostic testing) it is recommended to increase the total daily dose by 0.5 mg increments (if the drug is tolerated at that dose) every 4-6 weeks until stabilisation occurs. If signs of dose intolerance develop, treatment should be stopped for 2-3 days and reinstated at one-half of the previous dose. The total daily dose may then be titrated back up to the desired clinical effect by 0.5 mg increments every 2-4 weeks. If a dose is missed, the next scheduled dose should be administered as prescribed.
Following stabilisation, regular clinical assessment and diagnostic testing should be performed every 6 months to monitor treatment and dose. Where there is no apparent response to treatment, the diagnosis should be re-evaluated.
Withdrawal periods
Not authorised for use in horses intended for human consumption.
Treated horses may never be slaughtered for human consumption.
The horse must have been declared as not intended for human consumption under national horse passport legislation.
Not authorised for use in mares producing milk for human consumption.
Pharmacological particulars
ATCvet code: QN04BC02
Pharmacodynamic properties
Pergolide is a synthetic ergot derivative and is a potent, long-acting dopamine receptor agonist. Both in vitro and in vivo pharmacological studies have demonstrated the activity of pergolide as a selective dopamine agonist with little or no effect on norepinephrine, epinephrine or serotonin pathways at therapeutic doses. As with other dopamine agonists, pergolide inhibits the release of prolactin. In horses with Pituitary Pars Intermedia Dysfunction (PPID) pergolide exerts its therapeutic effect by stimulating dopamine receptors. Further, in horses with PPID, pergolide has been shown to decrease the plasma levels of ACTH, MSH and other pro-opiomelanocortin peptides.
Pharmacokinetic properties
Pharmacokinetic information in the horse is available for oral doses of 2, 4 and 10 µg pergolide/kg body weight. It has been demonstrated that pergolide is rapidly absorbed with a short time to peak concentration.
Peak concentrations (Cmax) following the dose of 10 µg/kg were low and variable with a mean of ~ 4 ng/ml and a mean terminal half-life (T ½) of ~ 6 hours. The median time of peak concentration (Tmax) was ~ 0.4 hours and the area under the curve (AUC) was ~ 14 ng x hours/ml.
In a more sensitive analytical assay, plasma concentrations following the dose of 2 µg pergolide/kg were very low and variable with peak concentrations ranging from 0.138-0.551 ng/ml. The peak concentrations occurred at 1.25+/-0.5 hours (Tmax). Plasma concentrations in most horses were quantifiable for only 6 hours post dose. However, one horse had quantifiable concentrations for 24 hours. Terminal half-lives were not calculated as there was incomplete elucidation of the plasma concentration-time curve for most horses.
Peak concentrations (Cmax) following the dose of 4 µg/kg were low and variable with a range from 0.4–4.2 ng/mL with a mean of 1.8 ng/mL, and a mean terminal half-life (T ½) of ~ 6 hours. The median time of peak concentration (Tmax) was ~ 0.6 hours and the AUCt ~ 3.4 ng x h/ml.
Pergolide mesilate is approximately 90% associated with plasma proteins in humans and laboratory animals. The route of elimination is via the kidneys.
Pharmaceutical particulars
Shelf life
Shelf life of the veterinary medicinal product as packaged for sale: 30 months
Special precautions for storage
Store in the original package, in order to protect from light.
Immediate packaging
PVC/PE/PVDC-aluminium blister containing 10 tablets.
OPA/aluminium/PVC-aluminium blister containing 10 tablets.
Carton box of 10, 30, 60, 90, 100, 120, 160 or 240 tablets.
Not all pack sizes may be marketed.
Disposal
Medicines should not be disposed of via wastewater or household waste.
Use take-back schemes for the disposal of any unused veterinary medicinal product or waste materials derived thereof in accordance with local requirements and with any national collection systems applicable to the veterinary medicinal product concerned.
Horses (non-food producing)
Indications for use
Symptomatic treatment of clinical signs associated with Pituitary Pars Intermedia Dysfunction (PPID) (Equine Cushing's Disease).
Contraindications
Do not use in horses with known hypersensitivity to pergolide mesilate or other ergot derivatives or to any of the excipients.
Do not use in horses less than 2 years of age.
Special warnings
Appropriate endocrinologic laboratory tests should be conducted as well as evaluation of clinical signs in order to establish a diagnosis of PPID.
Special warnings for use in the target species
As the majority of cases of PPID are diagnosed in aged horses, other pathological processes are frequently present. For monitoring and frequency of testing, see Amounts to be administered and administration route.
Special precautions to be taken by the person administering the veterinary medicinal product to animals
This product may cause hypersensitivity (allergy) reactions. People with known hypersensitivity to pergolide or other ergot derivatives should avoid contact with the veterinary medicinal product.
This product may cause adverse effects due to decreased prolactin levels, which poses a particular risk to pregnant and lactating women. Pregnant or lactating women should avoid dermal contact or hand-to-mouth contact and wear gloves when administering the product.
Accidental ingestion, especially by children, may cause adverse reactions such as emesis, dizziness, lethargy or low blood pressure. To avoid accidental ingestion, the blister should be replaced into the carton and carefully kept away from children. Avoid hand-to-mouth contact. Do not eat, drink or smoke when using this product. In case of accidental ingestion, seek medical advice immediately and show the package leaflet or the label to the physician.
This product may cause eye irritation. Avoid contact with the eyes including hand-to-eye contact when handling the tablets. Minimize exposure risks when dissolving the tablets, e.g. tablets should not be crushed. In case of contact of the dissolved product with skin, wash exposed skin with water. In the event of eye exposure, flush the affected eye immediately with water and seek medical advice.
Wash hands after use.
Adverse reactions
Horses:
Rare (1 to 10 animals / 10,000 animals treated):
Inappetence, anorexia1, lethargy1. Central nervous system signs2 (e.g. depression2, ataxia2) . Diarrhoea, colic.
Very rare (<1 animal / 10,000 animals treated, including isolated reports):
Sweating.
1 transient
2 mild
Reporting adverse events is important. It allows continuous safety monitoring of a veterinary medicinal product. Reports should be sent, preferably via a veterinarian, to either the marketing authorisation holder or its local representative or the national competent authority via the national reporting system. See also section ‘contact details' of the package leaflet for respective contact details.
Use during pregnancy and lactation
Pregnancy: Use only according to the benefit/ risk assessment by the responsible veterinarian. The safety of this veterinary medicinal product has not been demonstrated in pregnant mares. Laboratory studies in mice and rabbits have not produced any evidence of teratogenic effects. Reduced fertility was seen in mice at a dose of 5.6 mg/kg body weight per day.
Lactation: The use is not recommended in lactating horses, in which the safety of this veterinary medicinal product has not been demonstrated. In mice, reduced body weights and survival rates in the progeny were attributed to the pharmacological inhibition of prolactin secretion resulting in lactation failure.
Interactions
Use with caution in case the veterinary medicinal product is co-administered with other drugs known to affect protein binding.
Do not administer concurrently with dopamine antagonists, such as neuroleptics (phenothiazines - e.g. acepromazine), domperidone, or metoclopramide, as these agents may reduce the effectiveness of pergolide.
Amounts to be administered and administration route
Oral use, once daily.
To facilitate administration, the required daily dose should be placed in a small amount of water and/or mixed with molasses or other sweetener and agitated until dissolved. In this case, the dissolved tablets should be administered with a syringe.
The whole amount should be administered immediately. Tablets should not be crushed, see Special precautions to be taken by the person administering the veterinary medicinal product to animals.
Starting dose:
The starting dose is about 2 µg pergolide/kg (dose range: 1.3-2.5 µg/kg; see table below). The maintenance dose should then be titrated according to the individual response as determined by monitoring (see below), resulting in an average maintenance dose of 2 µg pergolide/kg body weight with a dose range of 0.6-10 µg pergolide/kg body weight.
Starting doses are recommended as follows:
Horse body weight
0.5 mg tablet
1 mg tablet
2 mg tablet
Starting dose
Dosage range
200-400 kg
O
0.5 mg
1.3-2.5 µg/kg
401-600 kg
O
1.0 mg
1.7-2.5 µg/kg
OR
401-600 kg
OO
1.0 mg
1.7-2.5 µg/kg
601-850 kg
O
+
O
1.5 mg
1.8-2.5 µg/kg
OR
601-850 kg
OOO
1.5 mg
1.8-2.5 µg/kg
851-1000 kg
O
2.0 mg
2.0-2.4 µg/kg
OR
851-1000 kg
OO
2.0 mg
2.0-2.4 µg/kg
Maintenance dose:
Lifelong treatment is anticipated for this disease.
Most horses respond to therapy and are stabilised at an average dose of 2 µg pergolide/kg body weight. Clinical improvement with pergolide is expected within 6-12 weeks. Horses may respond clinically at lower or varying doses; it is therefore recommended to titrate to the lowest effective dose per individual based on response to therapy, whether it is effectiveness or signs of intolerance. Some horses may require doses as high as 10 µg pergolide/kg body weight per day. In these rare situations, appropriate additional monitoring is advised.
Following initial diagnosis, repeat endocrinologic testing for dose titration and monitoring of treatment at intervals of 4-6 weeks until stabilisation or improvement of clinical signs and/or diagnostic testing occurs.
If clinical signs or diagnostic testing have not yet improved at the first 4-6 week interval, the total daily dose may be increased by 0.50 mg. In case clinical signs have improved but are not yet normalised, the veterinarian may decide to titrate or not to titrate the dose, considering the individual's response/tolerance to the dose.
In case clinical signs are not adequately controlled (clinical evaluation and/or diagnostic testing) it is recommended to increase the total daily dose by 0.5 mg increments (if the drug is tolerated at that dose) every 4-6 weeks until stabilisation occurs. If signs of dose intolerance develop, treatment should be stopped for 2-3 days and reinstated at one-half of the previous dose. The total daily dose may then be titrated back up to the desired clinical effect by 0.5 mg increments every 2-4 weeks. If a dose is missed, the next scheduled dose should be administered as prescribed.
Following stabilisation, regular clinical assessment and diagnostic testing should be performed every 6 months to monitor treatment and dose. Where there is no apparent response to treatment, the diagnosis should be re-evaluated.
Withdrawal periods
Not authorised for use in horses intended for human consumption.
Treated horses may never be slaughtered for human consumption.
The horse must have been declared as not intended for human consumption under national horse passport legislation.
Not authorised for use in mares producing milk for human consumption.
Pharmacological particulars
ATCvet code: QN04BC02
Pharmacodynamic properties
Pergolide is a synthetic ergot derivative and is a potent, long-acting dopamine receptor agonist. Both in vitro and in vivo pharmacological studies have demonstrated the activity of pergolide as a selective dopamine agonist with little or no effect on norepinephrine, epinephrine or serotonin pathways at therapeutic doses. As with other dopamine agonists, pergolide inhibits the release of prolactin. In horses with Pituitary Pars Intermedia Dysfunction (PPID) pergolide exerts its therapeutic effect by stimulating dopamine receptors. Further, in horses with PPID, pergolide has been shown to decrease the plasma levels of ACTH, MSH and other pro-opiomelanocortin peptides.
Pharmacokinetic properties
Pharmacokinetic information in the horse is available for oral doses of 2, 4 and 10 µg pergolide/kg body weight. It has been demonstrated that pergolide is rapidly absorbed with a short time to peak concentration.
Peak concentrations (Cmax) following the dose of 10 µg/kg were low and variable with a mean of ~ 4 ng/ml and a mean terminal half-life (T ½) of ~ 6 hours. The median time of peak concentration (Tmax) was ~ 0.4 hours and the area under the curve (AUC) was ~ 14 ng x hours/ml.
In a more sensitive analytical assay, plasma concentrations following the dose of 2 µg pergolide/kg were very low and variable with peak concentrations ranging from 0.138-0.551 ng/ml. The peak concentrations occurred at 1.25+/-0.5 hours (Tmax). Plasma concentrations in most horses were quantifiable for only 6 hours post dose. However, one horse had quantifiable concentrations for 24 hours. Terminal half-lives were not calculated as there was incomplete elucidation of the plasma concentration-time curve for most horses.
Peak concentrations (Cmax) following the dose of 4 µg/kg were low and variable with a range from 0.4–4.2 ng/mL with a mean of 1.8 ng/mL, and a mean terminal half-life (T ½) of ~ 6 hours. The median time of peak concentration (Tmax) was ~ 0.6 hours and the AUCt ~ 3.4 ng x h/ml.
Pergolide mesilate is approximately 90% associated with plasma proteins in humans and laboratory animals. The route of elimination is via the kidneys.
Pharmaceutical particulars
Shelf life
Shelf life of the veterinary medicinal product as packaged for sale: 30 months
Special precautions for storage
Store in the original package, in order to protect from light.
Immediate packaging
PVC/PE/PVDC-aluminium blister containing 10 tablets.
OPA/aluminium/PVC-aluminium blister containing 10 tablets.
Carton box of 10, 30, 60, 90, 100, 120, 160 or 240 tablets.
Not all pack sizes may be marketed.
Disposal
Medicines should not be disposed of via wastewater or household waste.
Use take-back schemes for the disposal of any unused veterinary medicinal product or waste materials derived thereof in accordance with local requirements and with any national collection systems applicable to the veterinary medicinal product concerned.
Shipping charges mainland GB zone1
| Value | Weight | Delivery Charge |
| Over £49.00 | Any Weight | FREE |
| Under £49.00 | No weight limit | £4.50 |
| Under £49.00 | Under 250 grams | £3.49 |
Most orders are despatched the same day and standard delivery is 3 to 5 working days from despatch. FAST Expedited options are available at extra cost - these usually arrive in 24-48hrs from dispatch but delays are possible during busy periods.
Postcodes outside of Zone 1 (including some areas within mainland UK) may incur extra carriage charges due to surcharges imposed by the couriers. These will be calculated on the website at the checkout.
NB: Orders placed with faster delivery must be placed before 13:00 to ensure same day dispatch (excluding weekends and bank holidays). Please also check on the product page that the items ordered show 'In Stock' otherwise your order will be delayed until the stock becomes available, which in most cases will only be 24hrs.
Estimated "Usually shipped in" information is shown against most products
Overseas orders
We no longer send goods outside of the UK.
Prescription Items
Prescription items will be sent on receipt of a valid signed and dated prescription.
Pick up
We offer a pickup service for orders placed over the phone.
Please ring us on 01833 641112 for more information.
Refrigerated Items
Refrigerated items will be sent by carrier or express delivery at a cost of £7.50, with coolpacks, unless you pay for a premium for a refrigerated delivery. We will contact you prior to despatch for your instructions.
We want you to be completely satisfied with any purchase. If not any item* can be returned to us within 14 days of receipt for exchange or refund Please give us a ring for a returns number on 01833 641112 or alternatively email sales@hyperdrug.co.uk to obtain a returns number.
*Due to legal requirements medicines may not be returned except to correct an error in despatch or in response to an "official recall". If an item is believed to be faulty it should be returned for inspection and it may be necessary to forward it to the manufacturers for testing before replacements or refunds can be authorised. This does not infringe legal rights. Please contact our customer services for a "Returns Number" which must appear on the outside of the package or it will not be accepted. We advise customers to use an insured method of shipping and to retain proof of despatch. We may refuse returns on products specially obtained or manufactured to order. Items must be returned unsoiled and unused and sent adequately packed and carriage paid.
