EX-7.5 suspension for oral use

Product benefits:

• Patented.
• Innovative technologies.
• High quality megestrol acetate substance provides high bioavailability, efficiency and safety of the drug.
• Available for females and males.

Chemical composition and pharmacological properties

1 ml of EX-5 contains megestrol acetate - 20 mg as an active ingredient. 1 ml of EX-7.5 contains megestrol acetate - 30 mg. 1 0.05 g tablet of EX-5Т contains megestrol acetate - 5 mg.
Pharmacological group: hormones and their antagonists.
Megestrol acetate (an active ingredient of EX drugs) effects on hypotalamo-pituitary system and blocks gonadotrope (FSH and LH) secretion providing antiestrogenic and antiovulatory action to animal gonades causing estral inhibition. Megestrol acetate also provides significant antiglucocorticoid activity.
Megestrol acetate well absorbs from gastrointestinal tract with further hepatic metabolization to conjugates and is excreted as metabolites in urine and feces. After the drug withdrawal 90% of total dose is excreted within 15 days.

Indications

Use EX in female dogs and cats to interrupt or detain estrus (to move it in time) in order to avoid random mating or adverse offspring; in male dogs and cats to decrease sexual activity, correct behaviour problems during estrus (decreases aggression, hyperexcitability, hypersexuality and reduces marking territory habit). Use EX-5T in cats and small dogs. Dose depends on animal sex and administration purpose.

Contraindications

Increased individual sensitivity to the drug components.
These drugs are contraindicated for animals with genital system diseases (pyometra, metritis, endometritis etc.), breast tumors, diabetes, immature animals, pregnant and lactating females.
Drug administration is not recommended for young animals in the first estrus due to difficulty in sexual cycle beginning determination.

Adverse events

Adverse events and complications generally are not observed in case of EX administration as per package insert. In case of long-term or repeated administration, character change (aggression or depression), growth of breasts and appetite, associated body weight increase may be observed.

Dosage and administration

Suspensions are intended for oral administration in drops; tablets are intended for forced administration on the base of tongue or powdered with small amount of treat (1-2 hours before the main feeding).
Note dates of estrus beginning and start of drug administration.

Before use shake a bottle (tube or pipette) with EX-5 or EX-7.5 within a minute to homogenous suspension.

Table 1

Indications	Megestrol acetate dose	Dosage EX-5	Dosage EX-7.5	Start of administration	Course of use duration
To detain estrus in female cats	2.5 mg every week or 5 mg once in every 2 weeks.	4 drops (0.125 ml) every week or 8 drops (0.25 ml) once in every 2 weeks.	2-3 drops (0.09 ml) every week or 5 drops (0.17 ml) once in 2 weeks.	During anestrum beyond parturiating season. Do not use the drug in pregnant animals.	Use up to 18 months in succession. Before the beginning of other course of use it is recommended to wait for normal physiological cycle (estrus).
To interrupt estrus in female cats	5 mg every day	8 drops (0.25 ml) every day	5 drops (0.17 ml) every day	Within 3 days after the first estral signs	Within 5-7 days until estral signs disappear. It is recommended to interrupt estrus not more than twice a year.
To decrease sexual activity and correct adverse behaviour in male cats	5 mg every day	8 drops (0.25 ml) every day	5 drops (0.17 ml) every day		Within 5-7 days, then administer the same dose (5 mg) once a week. It is recommended to use drugs in the light of animal behaviour modification.

Table 2

Indications	Start of administration	Daily megestrol acetate dose per 1 kg of body weight	EX-5 daily dose	EX-7.5 daily dose	Course of use duration
To detain estrus in female dogs	Within 7-15 days before estrus beginning	0.5 mg/kg	4 drops (0.125 ml) per every 5 kg of body weight	The longest course of use is 32 days. Administer within a term of desirable estrus detainment. Only 2 courses of use are recommended within a year.	Estrus may start in a few days after the drug withdrawal. In case of long-term drug administration (about a month), estrus starts in 2-9 or often in 3-6 months.
To interrupt estrus in female dogs	Within 3 days after the estrus beginning	2 mg/kg	15 drops (0.5 ml) per every 5 kg of body weight	Administer daily dose during the first 3 days of course, then use half of this dose within following 7 days. Only 2 courses of use are recommended within a year.	Next estrus beginning is individual for every female dog depending on drug administration time. Usually estrus starts in 2-9 or often in 3-6 months.
To decrease sexual activity and correct adverse behaviour in male dogs		2 mg/kg	15 drops (0.5 ml) per every 5 kg of body weight	The first course lasts within a week (daily administration). In case of positive result, administer a half-dose (1 mg/kg) every day within 2 weeks.	It is recommended to use the drug in the light of animal behaviour modification.

To detain estrus in female cats administer EX-5T by 1 tablet once in 2 weeks or a half of tablet every week during anestrum. The course lasts up to 18 months. Before beginning of the other one it is recommended to wait for normal feline physiological cycle (estrus).

In order to interrupt feline estrus, within 3 days after the estrus beginning administer 1 tablet every day within 5-7 days until estral signs disappear. It is recommended to interrupt estrus not more than twice a year.

If estrus beginning is difficult to be determined in several female cats, you would rather detain it than interrupt.

In order to decrease sexual activity and correct adverse behaviour in male cats (urine marking territory, intraspecific aggression, tendency to vagrancy, hyperexcitability), use 1 tablet of EX-5T once a day within 5-7 days, then once a week till behaviour correction.

In order to detain estrus in female dogs, administer 0.5 mg of megestrol acetate per 1 kg of body weight in a day within 7-15 days before estrus beginning. In the light of body weight, dosage is listed in Table 3. Administration duration depends on desired date of estrus detainment (up to 32 days). Estrus may start in a few days after the drug withdrawal. In case of long-term drug administration (about a month), estrus usually starts in 4-6 or sometimes in 2-9 months. Only two courses of use are recommended within a year.

Table 3

	Megestrol acetate daily dose, mg	EX-5T daily dose, tablets
<5	2.5	0.5
6-10	5	1
11-15	7.5	1.5
16-20	10	2
21-30	15	3
31-40	20	4

In case of the first estral signs (bloody discharge), administer 2 mg of megestrol acetate per 1 kg of body weight in a day to interrupt estrus in female dogs within 3 days after the estrus beginning Administer daily dose within the first 3 days, then use half-dose within following 7 days. After the drug withdrawal estrus usually starts in 4-6 months or sometimes in 2-9 months. Only two courses of use are recommended within a year.

Table 4

Body weight, kg	Megestrol acetate daily dose, mg	EX-5T daily dose, tablets
<5	10	2
6-10	20	4
11-15	30	6
16-20	40	8
21-30	60	12
31-40	80	16

In order to decrease sexual activity and correct adverse behaviour in male dogs (indoor urine marking territory, hyperexcitability), every day administer 2 mg of megestrol acetate per 1 kg of body weight within a week. In case of positive result, administer a half-dose within 2 weeks.

Special warnings

EX drugs are incompatible with nonhormonal drugs and feed supplements. Long-term combined administration with corticosteroids is not recommended.

Storage

Store EX drugs in closed original package. Protect from direct sunlight and moisture. Store separately from food and animal feeding at 5-30°С.

Shelf lives of emulsions and tablets are 2 and 3 years from manufacturing date, respectively, when stored in accordance with regulations.

Do not use after shelf life termination.

Pharmaceutical form

EX-5 and EX-7.5 are manufactured in 2 ml and 3 and 5 ml polymeric dropper bottles, respectively; 10 tablets in blister with a package insert packed in cartons.