Brimonidine-AFT

Country: New Zealand

Language: English

Source: Medsafe (Medicines Safety Authority)

Active ingredient:

Brimonidine tartrate 2 mg/mL;  

Available from:

AFT Pharmaceuticals Ltd

INN (International Name):

Brimonidine tartrate 2 mg/mL

Dosage:

0.2% w/v

Pharmaceutical form:

Eye drops, solution

Composition:

Active: Brimonidine tartrate 2 mg/mL   Excipient: Benzalkonium chloride Citric acid Polyvinyl alcohol Purified water Sodium chloride Sodium citrate dihydrate Sodium hydroxide

Units in package:

Bottle, dropper, 10cc white plastic round (LDPE),dropper tip-15mm white plastic (LDPE),dropper tip cap-white plastic, 5 mL

Class:

Prescription

Prescription type:

Prescription

Manufactured by:

Farmak a.s.

Product summary:

Package - Contents - Shelf Life: Bottle, dropper, 10cc white plastic round (LDPE),dropper tip-15mm white plastic (LDPE),dropper tip cap-white plastic - 5 mL - 36 months from date of manufacture stored at or below 25°C 4 weeks opened stored at or below 25°C

Authorization date:

2003-08-22

Summary of Product characteristics

BRIMONIDINE AFT 
_Brimonidine tartrate 0.2%w/v Ophthalmic solution _

PRESENTATION 
BRIMONIDINE-AFT  is  a  clear,  greenish-yellow  sterile  ophthalmic  solution  containing 
brimonidine tartrate  0.2% (2mg/mL) 

USES 
_ACTIONS _
Brimonidine is an alpha-2 adrenergic agonist that is 1000-fold more selective for the alpha-2 
adrenoreceptor  than  the  alpha-1  adrenoreceptor.  Affinity  at  human  alpha-1  and  alpha-2 
adrenoreceptors  are  ~2000  nM  and  ~2  nM,  respectively.  This  selectivity  results  in  no 
mydriasis and the absence of vasoconstriction in microvessels associated with human retinal 
xenografts. 
Topical administration of BRIMONIDINE-AFT eye drops decreases intraocular pressure (IOP) 
in  humans.  When  used  as  directed,  BRIMONIDINE-AFT  eye  drops  have  the  action  of 
reducing elevated IOP with minimal effect on cardiovascular
parameters. 
BRIMONIDINE  eye  drops  have  a  rapid  onset  of  action,  with  the  peak  ocular  hypotensive 
effect
occurring at two hours post-dosing. The duration of effect
is 12 hours or greater. 
Fluorophotometric  studies  in  animals  and  humans  suggest  that  brimonidine  tartrate  has  a 
dual  mechanism  of  action.  BRIMONIDINE-AFT  eye  drops  lower  IOP  by  reducing  aqueous 
humor production and enhancing uveoscleral outflow. 
_PHARMACOKINETICS _
After ocular administration of a 0.2% solution of bromonidine tartrate eye drops twice daily in 
humans  for  10  days,  plasma  concentrations  were  low  (mean  C
max
  0.06  ng/mL).  Plasma 
concentrations  peaked  within  1  to  4  hours  and  declined  with  a  systemic  half-life  of 
approximately 3 hours. 
In  humans,  systemic  metabolism  of  brimonidine  is  extensive;  bri