Caverject

Country: New Zealand

Language: English

Source: Medsafe (Medicines Safety Authority)

Active ingredient:

Alprostadil 6.15ug equivalent to 5 µg/ml after reconstitution.

Available from:

Pharmacia Limited Company trading as Pharmacia

INN (International Name):

Alprostadil 6.15 µg (=5 µg/ml after reconstitution.)

Dosage:

5 mcg

Pharmaceutical form:

Powder for injection

Composition:

Active: Alprostadil 6.15ug equivalent to 5 µg/ml after reconstitution. Excipient: Hydrochloric acid Lactose monohydrate Sodium citrate dihydrate Sodium hydroxide Benzyl alcohol Water for injection

Units in package:

Combination pack, 6x(vial+ diluent syringe),

Class:

Prescription

Prescription type:

Prescription

Manufactured by:

Pharmacia & Upjohn Company LLC

Product summary:

Package - Contents - Shelf Life: Combination pack, 6x(vial+ diluent syringe) -   - 24 months from date of manufacture stored at 2° to 8°C (Refrigerate, do not freeze) 48 hours reconstituted stored at or below 25°C 7 days reconstituted stored at 2° to 8°C (Refrigerate, do not freeze) 24 months from date of manufacture stored at or below 25°C 24 hours reconstituted (not refrigerated) stored at or below 25°C - Combination pack, 1x(vial+ diluent syringe) - 1 dose units - 24 months from date of manufacture stored at 2° to 8°C (Refrigerate, do not freeze) 48 hours reconstituted stored at or below 25°C 7 days reconstituted stored at 2° to 8°C (Refrigerate, do not freeze) 24 months from date of manufacture stored at or below 25°C 24 hours reconstituted (not refrigerated) stored at or below 25°C - Syringe, glass, 1x1ml - 1 mL - 24 months from date of manufacture stored at 2° to 8°C (Refrigerate, do not freeze) - Vial, glass, 1x5?g - 5 ?g - 24 months from date of manufacture stored at 2° to 8°C (Refrigerate, do not freeze)

Authorization date:

1993-02-16

Summary of Product characteristics

DATA SHEET
CAVERJECT
®
ALPROSTADIL
10 MICROGRAMS AND 20 MICROGRAMS POWDER FOR INJECTION
PRESENTATION
Caverject
is
a
white
crystalline
powder
containing
10 micrograms
or
20 micrograms
alprostadil in a 5 mL clear glass vial.
USES
ACTIONS
Alprostadil is the naturally occurring form of prostaglandin E
1
(PGE
1
). Alprostadil has a
wide variety of pharmacological actions; vasodilation and inhibition
of platelet aggregation
are among the most notable of these effects. In most animal species
tested, alprostadil
relaxed retractor penis and corpus cavernosum urethrae
_in vitro_
. Alprostadil also relaxed
isolated preparations of human corpus cavernosum and spongiosum as
well as cavernous
arterial segments contracted by either noradrenaline or PGF
2
α
_in vitro_
. In pigtail monkeys
(
_Macaca nemestrina_
), alprostadil increased cavernous arterial blood flow
_in vivo_.
The degree
and
duration
of
cavernous
smooth
muscle
relaxation
in
this
animal
model
was
dose-
dependent.
Alprostadil induces erection by relaxation of trabecular smooth muscle
and by dilation of
cavernosal arteries. This leads to expansion of lacunar spaces and
entrapment of blood by
compressing the venules against the tunica albuginea, a process
referred to as the corporal
veno-occlusive mechanism.
PHARMACOKINETICS
_ABSORPTION _
For the treatment of erectile dysfunction, alprostadil is administered
by injection into the
corpora cavernosa. The absolute bioavailability of alprostadil has not
been determined.
_DISTRIBUTION _
Following intracavernosal injection of 20 micrograms alprostadil, mean
peripheral plasma
concentrations of alprostadil at 30 and 60 minutes after injection (89
and 102 picograms/mL,
respectively) were not significantly greater than baseline levels of
endogenous alprostadil
(96 picograms/mL). Alprostadil is bound in plasma primarily to albumin
(81% bound) and to
a lesser extent
α
-globulin IV-4 fraction (55% bound). No significant binding to
erythrocytes
or white blood cells was observed.
_BIOTRANSFORMATION OR METABOLISM _
Alprostadil
is