Active ingredients: Terazosin
TERAPROST 2 mg tablets
TERAPROST 5 mg tablets
TERAPROST 10 mg tablets
Indications Why is Teraprost used? What is it for?
PHARMACOTHERAPEUTIC CATEGORY
Alpha-adrenergic receptor antagonists
THERAPEUTIC INDICATIONS
Functional disorders of the first phase of benign prostatic hypertrophy.
Contraindications When Teraprost should not be used
Teraprost is contraindicated:
In patients with known hypersensitivity to the active substance "terazosin", to other quinazolines (prazosin, doxazosin) or to any of the excipients.
In subjects with a history of orthostatic hypotension.
Patients with a history of micturition syncope should not be treated with alpha-blocking drugs.
Precautions for use What you need to know before taking Teraprost
Terazosin therapy requires regular clinical monitoring. The drug can cause hypotension. Particular attention must therefore be paid to the evaluation of the pressure of the subjects being treated.
Terazosin, like other alpha-blocking drugs, can cause lowering of blood pressure, episodes of lipothymia, orthostatic hypotension and syncope, especially associated with the first or first doses of therapy (first dose effect) or when the dosage is increased.
Similar effects can also occur if the therapy is interrupted for more than a few doses and then restarted.
Patients should be informed about the symptoms of orthostatic hypotension and advised to sit or lie down in these cases (see also sections "Special warnings - Effects on ability to drive and" use machines "and" Undesirable effects ").
Cases of syncope associated with rapid dose increases or the introduction of antihypertensive drugs have also been reported.
Therefore, any concomitant antihypertensive treatment should be initiated with caution.
The concomitant use of phosphodiesterase type 5 inhibitors (eg sildenafil, tadalafil, vardenafil) and Teraprost may lead to symptomatic hypotension in some patients. In order to minimize the risk of developing orthostatic hypotension, the patient should be stabilized on alpha-blocker treatment prior to initiating therapy with phosphodiesterase type 5 inhibitors.
Since the probability of such phenomena occurring can be substantially decreased by starting treatment with the lowest posology (1 mg) at bedtime and increasing the doses progressively, it is recommended to carefully follow the instructions given in the paragraph "Dose, method and time. of administration ".
To minimize the risk of orthostatic hypotension, patients should also be carefully monitored, especially at the start of therapy.
The patient should also be warned of the possible onset of these effects and advised on the measures to be taken to deal with them.
In the event of an episode described above, the patient should be placed in the supine position and treated - if necessary - with appropriate supportive measures.
More frequently, other symptoms associated with the decrease in blood pressure may occur, namely dizziness, dizziness, drowsiness and palpitations. Patients in occupations for whom the symptoms described may pose a potential risk should be treated with particular caution.
Warn the patient that if symptoms of a drop in blood pressure are felt, it is necessary to sit or lie down; whereas these symptoms are not always orthostatic in nature, pay close attention when they arise from a sitting or lying position.
After the first 12 hours after initiation of therapy, after dose escalation or after restart of treatment following interruption, patients should be informed of the possibility of syncopal and orthostatic symptoms and avoid driving or engaging in risky activities. (see also section "Special warnings" - Effects on ability to drive and use machines).
Due to its vasodilatory action, terazosin should be used with caution in patients with any of the following cardiac conditions.
- Pulmonary edema due to aortic or mitral stenosis;
- Severe heart failure;
- Right ventricular infarction caused by pulmonary embolism or pericardial effusion;
- Left ventricular infarction with low pressure.
Use in patients with hepatic insufficiency
As with all drugs metabolised in the liver, terazosin should be used with particular care in patients with impaired liver function. Since there are no data available in patients with severe hepatic dysfunction, it is recommended that their use be avoided in these cases.
Caution is also recommended when terazosin is administered concomitantly with drugs that may affect hepatic metabolism.
Interactions Which drugs or foods may change the effect of Teraprost
Tell your doctor or pharmacist if you have recently taken any other medicines, even those without a prescription.
In patients receiving terazosin plus ACE inhibitors or diuretics, the incidence of dizziness or related side effects was higher than in the total population of patients receiving terazosin in clinical trials.
Caution should be exercised when terazosin is administered with other antihypertensive agents (ACE inhibitors, beta-receptor blockers, calcium antagonists and diuretics) to avoid the possibility of significant hypotension. If terazosin is added to a diuretic or other antihypertensive agent, a reduction in dosage and a new titration may be necessary.
The concomitant use of phosphodiesterase type 5 inhibitors (eg sildenafil, tadalafil, vardenafil) and Teraprost may lead to hypotensive symptoms in some patients (see section "precautions for use").
The combined use of terazosin with other alpha-receptor blockers is not recommended.
Warnings It is important to know that:
In the event that dizziness, lightheadedness or palpitations become bothersome, notify the treating physician so that he or she may consider adjusting the dosage. Long-term administration of Terazosin did not produce any clinically significant changes in the main laboratory parameters (glycaemia, uricaemia, creatininemia, azotemia and transaminasemia); the drug can therefore be used in diabetic patients, hyperuricaemic patients and in the elderly.
You are advised to inform your ophthalmologist of your current or previous treatment with terazosin before undergoing cataract surgery (clouding of the lens). Terazosin may cause complications during the operation which can be treated if the specialist is " been warned in time.
Pregnancy and breastfeeding
The medicine is not intended for use in women.
Effects on ability to drive and use machines
Vertigo, lightheadedness or somnolence may occur in conjunction with the intake of the initial dose or in the event of missed doses and subsequent re-initiation of terazosin therapy. Patients should take into account the possible onset of such adverse effects and the circumstances where they could occur.
Avoid driving or performing hazardous work within approximately the first 12 hours after taking the initial dose or if the dose is increased.
Important information about some of the excipients
TERAPROST tablets contain lactose. In case of ascertained intolerance to sugars, contact your doctor before taking the medicine.
Dosage and method of use How to use Teraprost: Dosage
The generally effective dosage is between 5 and 10 mg administered once a day.The effective dosage should be achieved gradually, starting with 1 mg (1/2 divisible 2 mg tablet) to be taken in the evening before bedtime (starter dose).
Thereafter, at weekly or biweekly intervals, the daily dose can be doubled to 2 mg and increased to 5 mg or 10 mg (1 tablet of 5 mg or 10 mg) in a single daily administration.
Method of administration
After taking the starter dose, the patient should avoid abrupt changes in position or activities that may be affected by dizziness or fatigue. This is especially true for the elderly. This precaution must also be observed when the first tablet is taken at each dose increase. The following tablets of each strength can be taken in the morning.
If the administration of the drug is interrupted for several days, the resumption of treatment must be carried out in the same way starting from the starter dose (1 mg).
Kidney failure
Pharmacokinetic studies indicate that patients with impaired renal function do not require any changes in the recommended dosage.
Hepatic insufficiency
See "Precautions for use" section.
Children
Safety and efficacy criteria in children have not been established.
Senior citizens
Pharmacokinetic studies performed in the elderly indicate that no substantial modification of the recommended dosage is required. However, particular caution is required for dose titration of terazosin.
Overdose What to do if you have taken too much Teraprost
Should the administration of terazosin cause acute hypotension, cardiovascular support interventions are of primary importance. Restabilization of blood pressure and normalization of heart rate can be achieved by keeping the patient in the supine position. If this measure proves inadequate, the state of shock should be treated with mass expanders and, if necessary, vasopressors can be used later. Renal function should be monitored and general supportive measures applied as needed. Dialysis may not be beneficial as laboratory data indicate a high degree of binding of terazosin to proteins.
In case of accidental ingestion of excessive doses of the medicine, notify your doctor or go to the nearest hospital.
IF YOU HAVE ANY DOUBTS ABOUT THE USE OF THERAPROST, CONTACT YOUR DOCTOR OR PHARMACIST.
Side Effects What are the side effects of Teraprost
Like all medicines, TERAPROST can cause side effects, although not everybody gets them.
Terazosin, like other alpha-adrenergic receptor antagonists, can cause syncope. Syncopal manifestations occurred in a time interval ranging from 30 to 90 minutes starting from the initial dose of the drug. Syncope has occasionally occurred in association with rapid dose increases or the introduction of another antihypertensive agent.
Syncope is believed to be due to an excessive orthostatic hypotension effect; although occasionally, syncope episodes were preceded by signs of severe supraventricular tachycardia with heart rates of 120 to 160 beats per minute.
In the event of syncope, the patient must be lying down and assisted with supportive treatment as needed.
In the event that the patient moves quickly from a sitting or lying position to a standing position, episodes of dizziness, lightheadedness or fainting may occur. Patients should be advised of this and instructed to lie down as soon as such symptoms appear and then remain seated for a few minutes before getting up to prevent recurrence of such episodes.
These adverse events are self-limiting and, in most cases, do not recur after the initial period of therapy or during subsequent retesting.
In clinical studies, the incidence of orthostatic hypotensive events was higher in patients aged 65 years and older (5.6%) compared to those aged below 65 years (2.6%).
Reporting of adverse events with terazosin
The most common adverse events were asthenia, palpitations, nausea, peripheral edema, dizziness, somnolence, nasal congestion / rhinitis and amblyopia / blurred vision. In addition, the following cases have been reported: back pain, headache, tachycardia, orthostatic hypotension, syncope, edema, weight gain, pain in extremity, decreased libido, depression, nervousness, paraesthesia, dizziness, dyspnoea, sinusitis and impotence. .
Other adverse reactions reported in clinical trials or reported during marketing, but not clearly associated with the use of terazosin, include the following: chest pain, face edema, fever, abdominal pain, neck pain, shoulder pain, vasodilation, arrhythmia , constipation, diarrhea, xerostomia, dyspepsia, flatulence, vomiting, gout; arthralgia, arthritis, joint disorders, myalgia, anxiety, insomnia, bronchitis, epistaxis, flu symptoms, pharyngitis, rhinitis, cold symptoms, itching, rash, increased cough, sweating, impaired vision, conjunctivitis, tinnitus, urinary frequency, urinary tract infection and urinary incontinence found mainly in menopausal women. At least two cases of severe anaphylactoid reactions have been recorded concurrently with the administration of terazosin.
Post-marketing experience: There have been reports of thrombocytopenia and priapism. Atrial fibrillation has been reported; however, a cause and effect relationship has not been established.
Laboratory Tests: Small but significant decreases in hematocrit, hemoglobin, leukocytes, total protein content and albumin have been observed in controlled clinical trials. These laboratory results suggest the possibility of hemodilution. Treatment based on terazosin continued up to 24 months had no significant effect on prostate specific antigen (PSA) levels.
Compliance with the instructions contained in the package leaflet reduces the risk of undesirable effects. If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please inform your doctor or pharmacist.
Expiry and Retention
EXPIRY: see the expiry date indicated on the package
The expiry date refers to the intact product, correctly stored.
WARNING: Do not use the medicine after the expiry date indicated on the package.
Deadline "> Other information
COMPOSITION:
TERAPROST 2 mg tablets
Each tablet contains:
- Active ingredient: Terazosin hydrochloride 2H2O 2.374 mg equal to Terazosin base 2 mg;
- Excipients: Lactose, Corn starch, Talc, Magnesium stearate, E-110
TERAPROST 5 mg tablets
- Each tablet contains:
- Active ingredient: Terazosin hydrochloride 2H2O 5.935 mg equal to Terazosin base 5 mg;
- Excipients: Lactose, Corn starch, Talc, Magnesium stearate, E-132, E-110
TERAPROST 10 mg tablets
Each tablet contains:
- Active ingredient: Terazosin hydrochloride 2H2O 11.87 mg equal to Terazosin base 10 mg;
- Excipients: Lactose, E-132, Corn starch, Talc, Magnesium stearate
PHARMACEUTICAL FORM AND CONTENT
Tablet
TERAPROST 2 mg: Blister of 10 divisible tablets
TERAPROST 5 mg: Blister pack of 14 divisible tablets
TERAPROST 10 mg: Blister of 14 tablets
Source Package Leaflet: AIFA (Italian Medicines Agency). Content published in January 2016. The information present may not be up-to-date.
To have access to the most up-to-date version, it is advisable to access the AIFA (Italian Medicines Agency) website. Disclaimer and useful information.
01.0 NAME OF THE MEDICINAL PRODUCT -
THERAPIST
02.0 QUALITATIVE AND QUANTITATIVE COMPOSITION -
Each 2 mg tablet contains:
Active principle
Terazosin hydrochloride 2H2O 2.374 mg
equal to Terazosin base 2.00 mg
Each 5 mg tablet contains:
Terazosin hydrochloride 2H2O 5.935 mg
equal to Terazosin base 5.00 mg
Each 10 mg tablet contains:
Terazosin hydrochloride 2H2O 11.87 mg
equal to Terazosin base 10.00 mg
For the full list of excipients, see section 6.1
03.0 PHARMACEUTICAL FORM -
Tablet
04.0 CLINICAL INFORMATION -
04.1 Therapeutic indications -
Functional disorders of the first phase of benign prostatic hypertrophy.
04.2 Posology and method of administration -
Dosage
The generally effective dosage is between 5 mg and 10 mg administered once daily.
The effective dosage should be achieved gradually, starting with 1 mg (1/2 divisible 2 mg tablet) to be taken in the evening before bedtime (starter dose).
Subsequently, at weekly or bi-weekly intervals, the daily dose can be doubled to 2 mg and increased to 5 mg or 10 mg (1 tablet of 5 mg or 10 mg, in a single daily administration.
Method of administration
After taking the starter dose, the patient should avoid abrupt changes in position or activities that may be affected by dizziness or fatigue. This is especially true for the elderly. This precaution must also be observed when the first tablet is taken at each dose increase. The following tablets of each strength can be taken in the morning
If the administration of the drug is interrupted for several days, the resumption of treatment must be carried out in the same way, starting from the starter dose.
Kidney failure
Pharmacokinetic studies indicate that patients with impaired renal function do not require any changes in the recommended dosage.
Hepatic insufficiency
See section 4.4 Special warnings and precautions for use.
Children
Safety and efficacy criteria in children have not been established.
Senior citizens
Pharmacokinetic studies performed in the elderly indicate that no substantial modification of the recommended dosage is necessary. However, particular caution is required for dose titration of terazosin.
04.3 Contraindications -
THERAPOST is contraindicated:
In patients with hypersensitivity to the active substance "terazosin", to other quinazolines (prazosin, doxazosin) or to any of the excipients;
In subjects with a history of orthostatic hypotension.
Patients with a history of micturition syncope should not be treated with alpha-blocking drugs.
04.4 Special warnings and appropriate precautions for use -
Since prostate cancer and benign prostatic hypertrophy can cause the same symptoms, it is necessary to rule out the presence of prostate cancer before starting treatment with TERAPROST.
Terazosin therapy requires regular clinical monitoring.
The drug can cause hypotension. Particular attention must therefore be paid to the evaluation of the pressure of the subjects being treated.
Terazosin, like other alpha-blocking drugs, can cause lowering of blood pressure, episodes of lipothymia, orthostatic hypotension and syncope, especially associated with the first or first doses of therapy (first dose effect) or when the dosage is increased. .
Similar effects can also occur if the therapy is interrupted for more than a few doses and then restarted.
Cases of syncope associated with rapid dose increases or the introduction of antihypertensive drugs have also been reported. Therefore, any concomitant antihypertensive treatment should be initiated with caution.
The concomitant use of phosphodiesterase type 5 inhibitors (eg sildenafil, tadalafil, vardenafil) and TERAPROST may lead to symptomatic hypotension in some patients. In order to minimize the risk of developing orthostatic hypotension, the patient should be stabilized on alpha-blocker treatment prior to initiating therapy with phosphodiesterase type 5 inhibitors.
Since the probability of these phenomena occurring can be substantially decreased by starting treatment with the lowest posology (1 mg) at bedtime and increasing the doses progressively, it is recommended to carefully follow the instructions given in section 4.2 Posology and method of administration. .
Furthermore, to minimize the risk of orthostatic hypotension, patients should be carefully monitored, especially at the start of therapy.
The patient should be warned of the possible onset of these effects and advised on the measures to be taken to cope with them.
In the event of an episode described above, the patient should be placed in the supine position and treated - if necessary - with appropriate supportive measures.
More frequently, other symptoms associated with the decrease in blood pressure may occur, namely dizziness, dizziness, drowsiness and palpitations.
Patients in occupations for whom the symptoms described may pose a potential risk should be treated with particular caution.
Warn the patient that if symptoms of a drop in blood pressure are felt, it is necessary to sit or lie down; Considering that these symptoms are not always of an orthostatic nature, pay close attention when they arise from a sitting or lying position.
After the first 12 hours after initiation of therapy, after dose escalation or after restart of treatment following interruption, patients should be informed of the possibility of syncopal and orthostatic symptoms and avoid driving or engaging in risky activities. (See also section 4.7).
Due to its vasodilatory action, terazosin should be used with caution in patients with one of the following cardiac conditions:
pulmonary edema due to aortic or mitral stenosis;
severe heart failure;
right ventricular infarction caused by pulmonary embolism or pericardial effusion;
left ventricular infarction with low pressure.
Use in patients with hepatic insufficiency
As with all drugs metabolised in the liver, terazosin should be used with particular care in patients with impaired liver function. Since there are no data available in patients with severe hepatic dysfunction, it is recommended that their use be avoided in these cases.
Caution is also recommended when terazosin is administered concomitantly with drugs that may affect hepatic metabolism.
TERAPROST tablets contain lactose. Therefore the medicinal product should not be used in patients with rare hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption.
Long-term administration of Terazosin did not produce any clinically significant changes in the main laboratory parameters (glycaemia, uricaemia, creatininemia, azotemia and transaminaseemia); the drug can therefore be used in diabetic patients, hyperuricaemic patients and in the elderly.
During cataract surgery some patients, previously treated or treated with drugs containing tamsulosin, have developed the Floppy Iris Syndrome (IFIS - Intraoperative Floppy Iris Syndrome), a variant of the small pupil syndrome. There have been isolated cases. with other alpha-1 adrenergic antagonists and the possibility of a class effect cannot be excluded. The appearance of this syndrome may increase surgical complications during surgery, the surgeon should be aware of current or previous treatment with alpha-1 adrenergic antagonists.
04.5 Interactions with other medicinal products and other forms of interaction -
In patients receiving terazosin plus ACE inhibitors or diuretics, the incidence of dizziness or related side effects was higher than in the total population of patients receiving terazosin in clinical trials.
Caution should be exercised when terazosin is administered with other antihypertensive agents (ACE inhibitors, beta-receptor blockers, calcium antagonists and diuretics) to avoid the possibility of significant hypotension.If terazosin is added to a diuretic or other antihypertensive agent, a reduction in dosage and a new titration may be necessary.
The concomitant use of phosphodiesterase type 5 inhibitors (eg sildenafil, tadalafil, vardenafil) and TERAPROST may lead to hypotensive symptoms in some patients (see section 4.4).
The combined use of terazosin with other alpha-receptor blockers is not recommended.
04.6 Pregnancy and breastfeeding -
Not relevant. The medicine is not intended for use in women.
04.7 Effects on ability to drive and use machines -
Vertigo, lightheadedness or somnolence may occur in conjunction with the initial dose or in the event of missed doses and subsequent re-initiation of terazosin therapy. Patients should be warned about such possible adverse events and the circumstances under which may occur, to avoid driving or doing hazardous work approximately within the first 12 hours after taking the initial dose or if the dose is increased.
04.8 Undesirable effects -
Terazosin, like other alpha-adrenergic receptor antagonists, can cause syncope. Syncopal manifestations occurred in a time interval ranging from 30 to 90 minutes starting from the initial dose of the drug. Syncope has occasionally occurred in association with rapid dose increases or the introduction of an antihypertensive agent.
Syncope is believed to be due to an excessive orthostatic hypotension effect; although occasionally, syncope episodes were preceded by signs of severe supraventricular tachycardia with heart rates of 120 to 160 beats per minute.
In the event of syncope, the patient should be lying down and assisted with supportive treatment as needed.
In the event that the patient moves quickly from a sitting or lying position to a standing position, episodes of dizziness, lightheadedness or fainting may occur. Patients should be advised of this and instructed to lie down as soon as such symptoms appear and then remain seated for a few minutes before getting up to prevent recurrence of such episodes.
These adverse events are self-limiting and, in most cases, do not recur after the initial period of therapy or during subsequent retesting.
In clinical trials conducted on the indication of treatment of benign prostatic hypertrophy (BPH), the incidence of orthostatic hypotensive events was higher in patients aged 65 years and older (5.6%), compared to those under the age of 65 (2.6%).
Reporting of adverse events with terazosin
The most common adverse events were asthenia, palpitations, nausea, peripheral edema, dizziness, somnolence, nasal congestion / rhinitis and amblyopia / blurred vision.
In addition, the following cases have been reported: back pain, headache, tachycardia, orthostatic hypotension, syncope, edema, weight gain, pain in extremity, decreased libido, depression, nervousness, paraesthesia, dizziness, dyspnoea, sinusitis and impotence. .
Other adverse reactions reported in clinical trials or reported during marketing, but not clearly associated with the use of terazosin, include the following: chest pain, face edema, fever, abdominal pain, neck pain, shoulder pain, vasodilation, arrhythmia , constipation, diarrhea, xerostomia, dyspepsia, flatulence, vomiting, gout; arthralgia, arthritis, joint disorders, myalgia, anxiety, insomnia, bronchitis, epistaxis, flu symptoms, pharyngitis, rhinitis, cold symptoms, itching, rash, increased cough, sweating, impaired vision, conjunctivitis, tinnitus, urinary frequency, urinary tract infection and urinary incontinence found mainly in postmenopausal women.
At least two cases of severe anaphylactoid reactions have been recorded in conjunction with the administration of terazosin.
Post-marketing experience: cases of thrombocytopenia and priapism have been reported. Atrial fibrillation has been reported, however, a cause and effect relationship has not been established.
Lab test: Small but significant decreases in hematocrit, hemoglobin, leukocytes, total protein content and albumin have been observed in controlled clinical trials. These laboratory results suggest the possibility of haemodilution. terazosin continued for up to 24 months had no significant effect on prostate specific antigen (PSA) levels.
04.9 Overdose -
Should the administration of terazosin cause acute hypotension, cardiovascular support interventions are of primary importance. Restabilization of blood pressure and normalization of heart rate can be achieved by keeping the patient in the supine position. If this measure proves inadequate, the state of shock should be treated with mass expanders and, if necessary, vasopressors can be used later. Renal function should be monitored and general supportive measures applied as needed. Dialysis may not be beneficial as laboratory data indicate a high degree of binding of terazosin to proteins.
05.0 PHARMACOLOGICAL PROPERTIES -
05.1 "Pharmacodynamic properties -
Pharmacotherapeutic group: Alpha-adrenergic receptor antagonists, ATC code: G04CA3
TERAPROST (Terazosin Hydrochloride) is an alpha-1-adrenergic receptor blocking agent. Chemically it is a quinazoline derivative 1- (4-amino-6,7-dimethoxy-2-quinazolinyl) -4 - [(tetrahydro-2-furanyl) carbonyl] -piperazine, HCl, dihydrate.
Use in benign prostatic hyperplasia (BPH)
Some studies indicate that alpha1-adrenergic receptor antagonism is useful for improving urodynamics in patients with chronic bladder obstruction, such as benign prostatic hyperplasia.
Symptoms of benign prostatic hyperplasia (BPH) are mainly caused by the presence of an enlarged prostate and by the increased tone of the smooth muscle of the exit opening of the urinary bladder and prostate, which is regulated by alpha1-adrenergic receptors.
Terazosin has been shown in in vitro experiments to antagonize phenylephrine-induced contractions of human prostate tissue. In clinical studies it has been shown that terazosin is able to improve urodynamics and symptoms in patients with benign prostatic hyperplasia (BPH).
Administration of TERAPROST for periods longer than 6 months did not produce clinically significant changes attributable to the drug in the following laboratory parameters: glucose, uric acid, creatinine, BUN, liver function, electrolytes.
05.2 "Pharmacokinetic properties -
Absorption
Terazosin is well absorbed (80-100%). Terazosin has a minimal "first pass" effect and the nearly full dose of terazosin is available systemically. Peak plasma concentrations are reached approximately 1-2 hours after oral administration in the fasted state.
Bioavailability is not significantly affected by food intake.
Distribution
About 90-94% of terazosin binds to plasma proteins. Protein binding is independent of the total concentrations of the active ingredient.
Biotransformation
The major metabolites of terazosin are originated through demethylation and conjugation.
Elimination
Approximately 10% - 20% of orally administered terazosin is excreted unchanged in the urine and faeces, respectively.
Approximately 40% of the administered dose of terazosin is excreted in the urine and 60% in the faeces. The total elimination half-life is approximately 8-13 hours.
Linearity / non-linearity of pharmacokinetics
After oral administration of terazosin the AUC and Cmax increase in proportion to the dose over the recommended range (2-10 mg).
05.3 Preclinical safety data -
Carcinogenicity: Terazosin has been shown to produce benign tumors of the adrenal medulla in male rats when administered in high doses over a long period of time. No such events were observed in female rats or in similar studies in mice. The relevance of these findings in relation to the clinical use of the active principle on humans is not known.
There was no evidence of a genotoxic effect of terazosin from in vitro and in vivo studies on the mutagenic potential of the substance.
The oral LD50 in rats is equal to 5900 mg / kg in males and 6600 in females and was significantly higher than that relative to mice (3780 mg / kg in males and 4150 in females), but within the same species. no sex-related differences were noted.
Tests were carried out on beagle dogs treated with terazosin administered orally for one year at doses of 2, 4, 7 and 20 mg / kg / day. There were no lethal events, no changes in body weight, weight gain curve and food consumption were noted. Finally, there were no changes in behavior, nor signs of toxic effects attributable to the drug in question, with the exception of a transient eyelid ptosis found in females treated with 20 mg / kg / day.
At the autopsy examination no micro / macroscopic alterations of the organs examined were noted.
In animals, TERAPROST demonstrates an action of reducing peripheral vascular resistance, through the blocking of alpha-1 receptors.
In vitro studies have shown that TERAPROST antagonizes phenylephrine-induced contractions in human prostate tissue.
Although no teratogenic effects have been detected in animal experiments, safety criteria have not been established during pregnancy and lactation.
Furthermore, data from animal studies show that terazosin can increase the duration of pregnancy or inhibit childbirth.
06.0 PHARMACEUTICAL INFORMATION -
06.1 Excipients -
Each 2 mg tablet contains:
Excipients:
Lactose, Corn starch, Talc, Magnesium stearate, E-110
Each 5 mg tablet contains:
Excipients:
Lactose, Corn starch, Talc, Magnesium stearate, E-132, E-110
Each 10 mg tablet contains:
Excipients:
Lactose, E-132, Corn starch, Talc, Magnesium stearate.
06.2 Incompatibility "-
Not relevant
06.3 Period of validity "-
3 years
06.4 Special precautions for storage -
No special storage precautions
06.5 Nature of the immediate packaging and contents of the package -
The tablets are packed in opaque aluminum blisters of:
10 divisible tablets of 2 mg
14 divisible tablets of 5 mg
14 tablets of 10 mg
06.6 Instructions for use and handling -
No special instructions
07.0 HOLDER OF THE "MARKETING AUTHORIZATION" -
MALESCI Pharmacobiological Institute S.p.A. Bagno a Ripoli (FI)
08.0 MARKETING AUTHORIZATION NUMBER -
TERAPROST 2 mg tablets - 10 divisible tablets AIC N .: 028651014
TERAPROST 5 mg tablets - 14 divisible tablets AIC N .: 028651026
TERAPROST 10 mg tablets - 14 tablets AIC N .: 028651053
09.0 DATE OF FIRST AUTHORIZATION OR RENEWAL OF THE AUTHORIZATION -
TERAPROST 2 mg tablets - 10 divisible tablets 16/02/1993 02/2008
TERAPROST 5 mg included - 14 divisible tablets 16/02/1993 02/2008
TERAPROST 10 mg tablets - 14 tablets 19/12/2002 02/2008
10.0 DATE OF REVISION OF THE TEXT -
June 2009
