Overdose : מינון יתר

9 OVERDOSAGE
Human experience of acute overdose with PREZISTA/ritonavir is limited. Single doses up to 3200 mg of the oral solution of darunavir alone and up to 1600 mg of the tablet formulation of darunavir in combination with ritonavir have been administered to healthy volunteers without untoward symptomatic effects.
No specific antidote is available for overdose with PREZISTA. Treatment of overdose with PREZISTA consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient. If indicated, elimination of unabsorbed active substance is to be achieved by emesis or gastric lavage. In general gastric lavage should not be performed more than 1 hour after ingestion of an overdose

Administration of activated charcoal may also be used to aid in removal of unabsorbed active substance. Since PREZISTA is highly protein bound, dialysis is unlikely to be beneficial in significant removal of the active substance.

10 DESCRIPTION
PREZISTA (darunavir) is an inhibitor of the human immunodeficiency virus (HIV-1) protease.
PREZISTA (darunavir), in the form of darunavir ethanolate, has the following chemical name: [(1S,2R)-3-[[(4- aminophenyl) sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-carbamic acid (3R,3aS,6aR)hexahydrofuro[2,3-b] furan-3-yl ester monoethanolate. Its molecular formula is C27H37N3O7S • C2H5OH and its molecular weight is 593.73. Darunavir ethanolate has the following structural formula: 


Darunavir ethanolate is a white to off-white powder with a solubility of approximately 0.15 mg/mL in water at 20°C.

PREZISTA 75 mg tablets are available as white, caplet-shaped, film-coated tablets for oral administration.
PREZISTA 150 mg tablets are available as white, oval-shaped, film-coated tablets for oral administration.
PREZISTA 600 mg tablets are available as orange, oval-shaped, film-coated tablets for oral administration.
PREZISTA 400 mg is available as a light orange, oval-shaped, film-coated tablet for oral administration.
PREZISTA 800 mg tablets are available as dark red, oval-shaped, film-coated tablets for oral administration.

Each 75 mg tablet contains darunavir ethanolate equivalent to 75 mg of darunavir. Each 150 mg tablet contains darunavir ethanolate equivalent to 150 mg of darunavir. Each 400 mg tablet contains darunavir ethanolate equivalent to 400 mg of darunavir. Each 600 mg tablet contains darunavir ethanolate equivalent to 600 mg of darunavir. Each 800 mg tablet contains darunavir ethanolate equivalent to 800 mg of darunavir.

During storage, partial conversion from ethanolate to hydrate may occur; however, this does not affect product quality or performance.

Each 75mg 150mg 400mg 600mg tablet also contains the inactive ingredients colloidal anhydrous silica crospovidone, magnesium stearate, and PROSOLV SMCC. The 75 and 150 mg tablet film coating, OPADRY® White, contains polyethylene glycol 3350, polyvinyl alcohol-partially hydrolyzed, talc, and titanium dioxide. The 400 and 600 mg tablet film coating, OPADRY® Light Orange and OPADRY® Orange, respectively, contains
FD&C Yellow No. 6, polyethylene glycol, polyvinyl alcohol-partially hydrolyzed, talc, and titanium dioxide.

Each 800mg tablet also contain inactive ingredients: hypromellose 2910 15 mPa.s, silicified microcrystalline cellulose, crospovidone, colloidal silicon dioxide, magnesium stearate and OPADRY II DARK RED 85F150004 (contains polyvinyl alcohol-partially hydrolyzed, macrogol 3350, macrogol 4000, titanium dioxide, talc, iron oxide red.

All dosages for PREZISTA are expressed in terms of the free form of darunavir.