Procaine penicilline G hydrate is a composed of the β-lactam antibiotic of Penicillin G and the sodium channel blocker Procaine. As an antibiotic, Penicillin G is noted to posses effectiveness mainly against gram-positive organisms. Procaine Penicillin G is used a growth stimulant for poultry.
Antimicrobial activity
The procaine salt of benzylpenicillin. Poorly soluble (1:200 in
water). Administered intramuscularly as a suspension of crystals
which slowly dissolve at the site of the injection.
It must not be given intravenously. Intramuscular administration
produces a flat sustained plasma concentration of
penicillin, which is much lower than that achieved by an
equivalent dose of benzylpenicillin, with plasma levels still
detectable 24 h later. An injection of 0.6 g yields a peak plasma
concentration of 1–2 mg benzylpenicillin/L after 2–4 h. Free
procaine is detectable in the plasma within 30 min.
Very severe and potentially fatal reactions resembling those
of anaphylactic shock, but non-allergic in character, may
occur, probably due to accidental entry into the vascular system
at the site of injection and blockage of pulmonary and
cerebral capillaries by crystals of the suspension. Reactions
due to liberated procaine may include acute anxiety, hypertension,
tachycardia, vomiting, audiovisual hallucinations and
acute psychotic disturbance. The most severe reactions lead
to convulsions and cardiac arrest. Other reactions are those to
liberated benzylpenicillin.
