PW Lab 4

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Precompounded

pharmaceutical forms
prescriptions

• Prescriptions with antibacterial powders to be


reconstituted in the form of solutions for injectable
use – continued
• prescriptions of precoumponded products –
approximations for solid forms
Aciclovir, valaciclovir, penciclovir, famciclovir,
Prescribe acyclovir, brivudine, vidarabine are DNA polimerase
inhibitors, nucleosidic analogues. Their
commercial name mechanism of action is represented by the
Zovyrax®, so that the inhibition of ADN polimerases, after the
penetration into the host cell, and so the
patient should receive synthesis of some viral-specific structures is
20mg/kg daily, in three inhibited. Some of these are pro-drugs, being
equal daily doses, for 5 activated phosphorylation catalyzed by viral
thymidine to the active form. The activity
days. The vials contain spectrum includes Herpes simplex-1 virus,
either 500 mg or 1g. Herpes simplex-2 virus, varicela-zoster viruses.
The body weight of the Herpes simplex-2.

patient is 15kg.
The drug should be
administered
intramuscularly.
Adverse effects:

• Acyclovir, valacyclovir (prodrug, • after systemic administration of


metabolized with formation of acyclovir) acyclovir: nausea, diarrhea,
have also poor activity onvirusul Epstein-
Barr virus and cytomegaovirus, while headache, rash;
penciclovir and famciclovir (prodrug, • after topical administration: local
metabolized with formation of penciclovir) irritation, erythema;
have also poor activity on virus Epstein-
Barr and hepatitis B virus. Vidarabine is • high doses: neurotoxicity
also active on cytomegaovirus, (tremors, delirium);
rhabdoviruses, poxviruses, hepatis B virus,
oncogenes. • nephrotoxicity (to renal failure);
• In case of infections with Herpes simplex-1 • in immunocompromised patients:
virus, Herpes simplex-2 virus, varicela- sometimes lethal
zoster viruses, acyclovir is the drug of thrombocytopenia, hemolytic
choice (it is efficient on first onset and
recurrent oral herpes, genital herpes, uremic syndrome;
herpetic enkefalitis and infections with
varicela-zoster infections).
Prescribe acyclovir, Header
Rx/
commercial name Zovyrax®,
1. Zovyrax 0.5g
so that the patient should
Vials n. IV
receive 20mg/kg daily, in Label: Intramuscularly, use 2 mL from a vial
three equal daily doses, for 5 every 8 hours, for 5 days. Use four times
from one vial and then discard the unused
days. The vials contain either content.
500 mg or 1g. The body 2. Saline solution XmL
weight of the patient is 15kg. Ampoules n. IV
The drug should be Label: To reconstitute the antiviral
powder, use one ampoule for each vial.
administered intramuscularly. No refills!
Date Signature, Stamp
Prescribe cefuroxime, so
that the patient should
receive 75mg/kg daily, in
three equal daily doses,
for 5 days. The vials
contain either 750 mg or
1.5g. The body weight of
the patient is 100kg.
- of bacterial wall synthesis

Cephalosporins

A. first generation: C. third generation


- oral administration: cephradine, - oral administration: cefixime,
cefalexin, cefadroxil; cefpodoxime, ceftibuten;
- parenteral administration: - parenteral administration: ceftriaxone,
cephradine, cefazolin, cefalotin, ceftazidime, cefotaxime, cefoxitin,
cephapirin; cefoperazone, moxalactam,
B. second generation: ceftizoxime, ceftibuten, proxetil.
D. fourth generation - parenteral
- oral administration: cefuroxime,
administration: cefepime, cefpirome,
cefaclor, loracarbef, cefotiam;
cefclidine.
- parenteral administration:
C. fifth generation: - parenteral
cefuroxime, cefamandole, administration: ceftaroline,
cefmetazole, cefotetan, cefonicid, ceftobiprole.
ceforanid;
Header
Rx/
1. Cefuroxim 1.5g
Vials n. XXV
Label: Intravenously, 1 vial and 2/3 every 8
hours, for 5 days.
2. Saline solution XmL
Prescribe cefuroxime, so Ampoules n. XV
Label: To reconstitute the antibiotic powder,
that the patient should use 6mL from the ampoule for each vial.
receive 75mg/kg daily, in No refills!

three equal daily doses, Date Signature, Stamp

for 5 days. The vials


contain either 750 mg or
1.5g. The body weight of
the patient is 100kg.
Prescribe hydrocortisone
hemisuccinate, so that
the patient should
receive 2mg/kg daily, in
three equal daily doses,
for 3 days, intravenously
slowly, in infusion, in 3
hours time each infusion.
The body weight of the
patient is 75kg.
The ampoule contains
5mL and the
concentration is 5mg/mL.
On the prescription, we should
write:
1. The antibiotic: 2. The solvent
• in vials. • in ampouls.
The solvent can be:
a. saline solution: found in XmL
ampouls;
b. distilled water: found in XmL
ampouls or in VmL ampouls;
c. special solvent for lypophilic
susbtances: hydrocortisone
hemisuccinate: found in in VmL
ampouls with a 5mg/mL
concentration.
Glucocorticosteroids
Adverse reactions:
• characteristic changes of hyperadrenocorticism:
facies as "full moon", hirsutism, acne, stretch marks,
Classification fatty deposits on the trunk, but not members;
1. natural : cortisol, hydrocortisone; • the osteoporosis, loss of muscle mass;
2. synthetic: • the amenorrhea;
2.1. Short term / medium duration of action:
• sodium retention, hypertension, worsening of heart
hydrocortisone (hemisuccinate or acetate), failure;
prednisone, prednisolone, • dyslipidemia;
methylprednisolone, meprednisone; • the necrotizing arteritis rheumatic patients,
2.2. medium duration of action: worsening the damage of cartilage growth,
triamcinolone, paramethasone, • degeneration of the synovial folds;
fluprednisolone, beclometazone, • diabetes mellitus;
clobetazole, fluticazon, flunisolid, ciclesonid; • cataract, glaucoma;
2.3. long duration of action: betamethasone, • the gastro-intestinal ulcer;
dexamethasone. • immunosuppression → infections;
• psychotic symptoms;
• atrophy of the adrenal gland;
• stunting among children.
Calculus:
daily dose= 2mg/kg/day * 75kg = 150mg=0.15g
partial dose=(150mg/day):(3 administrations/day)=50mg=0.05g
Which is the amount of active substance in
one ampoule? So, there are needed 2 ampouls per 1pd (as
the pd=50 mg, and the ampoule contains
25mg).
1mL ____5mg=0.005g of hydrocortisone hemisuccinate
(active substance) It means a 10mL volume to be administered
each time.
5mL______? xg
x=25mg=0.025g Such a very small volume is totally unsuitable
for intravenously slowly, in infusion, in 3
hours time each infusion.
Thefore, we will use 1 vial of saline solution
of 500mL for an infusion.
So, we shouls also recommend 9 vials of
500mL of saline on the prescription.

Prescribe hydrocortisone hemisuccinate, so that the patient should receive


2mg/kg daily, in three equal daily doses, for 3 days, intravenously slowly, in
infusion, in 3 hours time each infusion. The body weight of the patient is 75kg.
The ampoule contains 5mL and the concentration is 5mg/mL.
Header
Rx/
Prescribe hydrocortisone 1. Hydrocortisone hemisuccinate 0.025g
hemisuccinate, so that Ampoules n. XVIII
the patient should Label: Intravenously slowly, in infusion, in 3 hours
time each infusion, 2 ampoules, 3 times per day, for
receive 2mg/kg daily, in 3 days.
three equal daily doses, 2. Saline solution 500g
for 3 days, intravenously Vials n. IX

slowly, in infusion, in 3 Label: As a vehicle for hydrocortisone


hemisuccinate, use one vial for 2 ampouls at each
hours time each infusion. administration.
The body weight of the No refills!

patient is 75kg. Date Signature, Stamp

The ampoule contains


5mL and the
concentration is 5mg/mL.
Prescribe ticlopidine,
Header
commercial name
Tiagren®, so that the Rx/
patient should receive Tiagren ___g
15mg/kg/day, in two equal Tablets n. ___
daily doses, for 7 days. The Label: Orally, ___, 2 times
tablets contain either per day, for 7 days.
No refills!
250mg or 500mg of the
Date Signature, Stamp
active substance. The
patient’s weight is 70 kg.
Calculus:
daily dose= 15mg/kg/day * 70kg = 1050mg=1.05g
partial dose=(1050mg/day):(2 administrations/day)=525mg=0.525g

pd = 525mg = 500mg + 25mg

we like we DISLIKE
Prescribe ticlopidine, Header
commercial name Rx/
Tiagren®, so that the Tiagren 0.5g
patient should receive
Tablets n. XIV
15mg/kg/day, in two equal Label: Orally, one tablet, 2
daily doses, for 7 days. The times per day, for 7 days.
tablets contain either No refills!
250mg or 500mg of the Date Signature, Stamp
active substance. The
patient’s weight is 70 kg.
Antitrombotics

Anticoagulants Antiplatele drugs


• parenteral route (unfractioned
heparin, low molecular weight Indications:
heparins), heparinoids • acute coronary syndrome (minor heart
attack or unstable angina);
(topical);
• thromboembolic stroke or transient
• antivitamines K (oral); ischemic attack;
• coronary artery bypass, bioprosthetic heart
• Direct or indirect inhibitors of: valve, stent in the arteries;
• trombin; • high cholesterol, high blood pressure,
• Xa factor; diabetes;
• prevention of thromboembolic accidents or
• others (very new); transient ischemic attacks in patients with
increased thrombotic risk (myocardial
infarction, unstable angina, stroke etc).
• in vitro.
Fibrinolytics
Antiplatelet drugs ---- bleeding
time need to be monitored. Adverse effects: promote bleeding;
• clopidogrel, ticagrelor and
prasugrel present less adverse
effects;
ticlopidine, clopidogrel, • for ticlopidine:
prasugrel, ticagrelor; • blood dyscrasias (leukopenia,
agranulocytosis, aplastic anemia),
increase in transaminases and
alkaline phosphatase,
antagonists on platelet hypercholesterolemia /
fibrinogen receptors: hypertriglyceridemia, skin
block the platelet receptor reactions;
for fibrinogen by inhibiting • metabolized by CYP2C19 --- great
individual variability.
binding of ADP-dependent
type;
Contraindications: in acute
hemorrhagic stroke,
thrombocytopenia.
Prescribe vigabatrin, Header
commercial name Sabril®, Rx/
so that the patient should Sabril ___g
receive 40mg/kg/day, in Tablets n. ___
two equal daily doses, for Label: Orally, ___, 2 times
7 days. The tablets per day, for 7 days.
contain either 500mg or No refills!
1g of the active Date Signature, Stamp
substance. The patient’s
weight is 18 kg.
Calculus:
daily dose= 40mg/kg/day *18 kg = 720mg=0.72g
partial dose=(720mg/day):(2 administrations/day)=360mg=0.36g
Prescribe vigabatrin, Header
commercial name Sabril®, Rx/
so that the patient should Sabril 0.5g
receive 40mg/day, in two Tablets n. XI
equal daily doses, for 7 Label: Orally, three quarters of
days. The tablets contain a tablet, 2 times per day, for 7 days.
either 500mg or 1g of the No refills!
Date Signature, Stamp
active substance. The
patient’s weight is 36 kg.

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