Tiepenem Actions

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Actions of Tiepenem in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Tiepenem (Imipenem (Tiepenem) and Cilastatin (Tiepenem) sodium, MSD) is a broad-spectrum β-lactam antibiotic supplied as IV infusion only. Tiepenem consists of 2 components: (1) Imipenem (Tiepenem), the 1st of a new class of β-lactam antibiotics, the thienamycins; and (2) Cilastatin (Tiepenem) sodium, a specific enzyme inhibitor that blocks the metabolism of Imipenem (Tiepenem) in the kidney, and substantially increases the concentration of intact Imipenem (Tiepenem) in the urinary tract. Imipenem (Tiepenem) and Cilastatin (Tiepenem) sodium are present in Tiepenem in a 1:1 ratio by weight.

The thienamycin class of antibiotics, to which Imipenem (Tiepenem) belongs, is characterized by a spectrum of potent bactericidal activity broader than that provided by any other antibiotic studied.

Microbiology: Tiepenem is a potent inhibitor of bacterial cell wall synthesis and is bactericidal against a broad spectrum of pathogens: Gram-positive and gram-negative, aerobic and anaerobic.

Tiepenem shares with the newer cephalosporins and penicillins a broad spectrum of activity against gram-negative species, but is unique in retaining the high potency against gram-positive species, previously associated only with earlier narrow-spectrum β-lactam antibiotics. The spectrum of activity of Tiepenem includes Pseudomonas aeruginosa, Staphylococcus aureus, Enterococcus faecalis and Bacteroides fragilis, a diverse group of problem pathogens commonly resistant to other antibiotics.

Tiepenem is resistant to degradation by bacterial β-lactamases, which makes it active against a high percentage of organisms eg, Pseudomonas aeruginosa, Serratia sp, and Enterobacter sp which are inherently resistant to most β-lactam antibiotics.

The antibacterial spectrum of Tiepenem is broader than that of any other antibiotic studied, and includes virtually all clinically significant pathogens. Organisms against which Tiepenem is usually active in vitro include: Gram-Negative Aerobes: Achromobacter sp; Acinetobacter sp (formerly Mima-Herellea); Aeromonas hydrophila; Alcaligenes sp; Bordetella bronchicanis; Bordetella bronchiseptica; Bordetella pertussis; Brucella melitensis; Campylobacter sp; Capnocytophaga sp; Citrobacter sp; Citrobacter diversus; Citrobacter freundii; Eikenella corrodens; Enterobacter sp; Enterobacter aerogenes; Enterobacter agglomerans; Enterobacter cloacae; Escherichia coli; Haemophilus ducreyi; Gardnerella vaginalis; Haemophilus influenzae (including β-lactamase-producing strains); Haemophilus parainfluenzae; Hafnia alvei; Klebsiella sp; Klebsiella oxytoca; Klebsiella ozaenae; Klebsiella pneumoniae; Moraxella sp; Morganella morganii (formerly Proteus morganii); Neisseria gonorrhoeae (including penicillinase-producing strains); Neisseria meningitidis; Pasteurella sp; Pasteurella multocida; Plesiomonas shigelloides; Proteus sp; Proteus mirabilis; Proteus vulgaris; Providencia sp; Providencia alcalifaciens; Providencia rettgeri (formerly Proteus rettgeri); Providencia stuartii; Pseudomonas sp**; Pseudomonas aeruginosa; Pseudomonas fluorescens; Pseudomonas pseudomallei; Pseudomonas putida; Pseudomonas stutzeri; Salmonella sp; Salmonella typhi; Serratia sp; Serratia proteamaculans (formerly Serratia liquefaciens); Serratia marcescens; Shigella sp; Yersinia sp (formerly Pasteurella); Yersinia enterocolitica; Yersinia pseudotuberculosis.

**Xanthomonas maltophilia (formerly Pseudomonas maltophilia) and some strains of Pseudomonas cepacia are generally not susceptible to Tiepenem.

Gram-Positive Aerobes: Bacillus sp; Enterococcus faecalis; Erysipelothrix rhusiopathiae; Listeria monocytogenes; Nocardia sp; Pediococcus sp; Staphylococcus aureus (including penicillinase-producing strains); Staphylococcus epidermidis (including penicillinase-producing strains); Staphylococcus saprophyticus; Streptococcus agalactiae; Streptococcus Group C; Streptococcus Group G; Streptococcus pneumoniae; Streptococcus pyogenes; Viridans group streptococci (including α- and γ-hemolytic strains).

Enterococcus faecium and methicillin-resistant are not susceptible to Tiepenem.

Gram-Negative Anaerobes: Bacteroides sp; Bacteroides distasonis; Bacteroides fragilis; Bacteroides ovatus; Bacteroides thetaiotaomicron; Bacteroides vulgatus; Bacteroides uniformis; Bilophila wadsworthia; Fusobacterium sp; Fusobacterium necrophorum; Fusobacterium nucleatum; Porphyromonas asaccharolyticus (formerly Bacteroides asaccharolyticus); Prevotella bivia (formerly Bacteroides bivius); Prevotella disiens (formerly Bacteroides disiens); Prevotella intermedia (formerly Bacteroides intermedius); Prevotella melaninogenica (formerly Bacteroides melaninogenicus); Veillonella sp.

Gram-Positive Anaerobes: Actinomyces sp; Bifidobacterium sp; Clostridium sp; Clostridium perfringens; Eubacterium sp; Lactobacillus sp; Microaerophilic streptococcus; Mobiluncus sp; Peptococcus sp; Peptostreptococcus sp; Propionibacterium sp (including P. acnes).

Others: Mycobacterium fortuitum; Mycobacterium smegmatis.

In vitro tests show Imipenem (Tiepenem) act synergistically with aminoglycoside antibiotics against some isolates of Pseudomonas aeruginosa.

How should I take Tiepenem?

This section provides information on the proper use of a number of products that contain Imipenem (Tiepenem) and Cilastatin (Tiepenem). It may not be specific to Tiepenem. Please read with care.

To help clear up your infection completely, Imipenem (Tiepenem) and Cilastatin (Tiepenem) combination must be given for the full time of treatment, even if you begin to feel better after a few days. Also, this medicine works best when there is a constant amount in the blood or urine. To help keep the amount constant, it must be given on a regular schedule.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Tiepenem administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Imipenem (Tiepenem) and Cilastatin (Tiepenem) is injected into a vein (IV) or into a muscle (IM).

Imipenem (Tiepenem) and Cilastatin (Tiepenem) is usually given in a clinic or hospital setting. The IV medicine must be given as a slow infusion and can take up to an hour to complete. Tell your caregiver if you feel nauseated during the infusion. You may need to receive the medicine at a slower rate.

The IM form of Imipenem (Tiepenem) and Cilastatin (Tiepenem) is given as a rapid injection into a muscle. You may be shown how to use injections at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

Tiepenem (for the muscle) and Primaxin IV (for the vein) are different forms of this medicine and should be used only for their specific type of injection. Do not inject Tiepenem into a vein and do not inject Primaxin IV into a muscle.

Imipenem (Tiepenem) and Cilastatin (Tiepenem) is usually given as long as needed until your infection has cleared or you have been symptom-free for at least 48 hours.

Use this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Imipenem (Tiepenem) and Cilastatin (Tiepenem) will not treat a viral infection such as the common cold or flu.

Do not give this medication to another person, even if they have the same symptoms you do.

Imipenem (Tiepenem) and Cilastatin (Tiepenem) is a powder that must be mixed with a liquid (diluent). Tiepenem and Primaxin IV are each mixed with different types of diluent.

Prepare your dose in a syringe only when you are ready to give yourself an injection.

After mixing Primaxin IV, you may keep it in a refrigerator and use it within 24 hours.

You may also store the mixed IV medicine at room temperature if you use it within 4 hours. Store unmixed Imipenem (Tiepenem) and Cilastatin (Tiepenem) powder at room temperature away from moisture and heat.

Tiepenem pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Following intramuscular administrations of 500 or 750 mg doses of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium in a 1:1 ratio with 1% lidocaine, peak plasma levels of Imipenem (Tiepenem) antimicrobial activity occur within 2 hours and average 10 and 12 µg/mL, respectively. For Cilastatin (Tiepenem), peak plasma levels average 24 and 33 g/mL, respectively, and occur within 1 hour. When compared to intravenous administration of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium, Imipenem (Tiepenem) is approximately 75% bioavailable following intramuscular administration while Cilastatin (Tiepenem) is approximately 95% bioavailable. The absorption of Imipenem (Tiepenem) from the IM injection site continues for 6 to 8 hours while that for Cilastatin (Tiepenem) is essentially complete within 4 hours. This prolonged absorption of Imipenem (Tiepenem) following the administration of the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium results in an effective plasma half- life of Imipenem (Tiepenem) of approximately 2 to 3 hours and plasma levels of the antibiotic which remain above 2 g/mL for at least 6 or 8 hours, following a 500 mg or 750 mg dose, respectively. This plasma profile for Imipenem (Tiepenem) permits IM administration of the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium every 12 hours with no accumulation of Cilastatin (Tiepenem) and only slight accumulation of Imipenem (Tiepenem).

A comparison of plasma levels of Imipenem (Tiepenem) after a single dose of 500 mg or 750 mg of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium (intravenous formulation) administered intravenously or of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium (intramuscular formulation) diluted with 1% lidocaine and administered intramuscularly is as follows:

PLASMA CONCENTRATIONS OF Imipenem (Tiepenem) (µg/mL)

TIME 500 MG 750 MG
I.V. I.M. I.V. I.M.
25 min 45.1 6.0 57.0 6.7
1 hr 21.6 9.4 28.1 10.0
2 hr 10.0 9.9 12.0 11.4
4 hr 2.6 5.6 3.4 7.3
6 hr 0.6 2.5 1.1 3.8
12 hr ND** 0.5 ND** 0.8
** ND: Not Detectable (<0.3 µg/mL)

Imipenem (Tiepenem) urine levels remain above 10 µg/mL for the 12-hour dosing interval following the administration of 500 mg or 750 mg doses of the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium. Total urinary excretion of Imipenem (Tiepenem) averages 50% while that for Cilastatin (Tiepenem) averages 75% following either dose of the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium.

Imipenem (Tiepenem), when administered alone, is metabolized in the kidneys by dehydropeptidase I resulting in relatively low levels in urine. Cilastatin (Tiepenem) sodium, an inhibitor of this enzyme, effectively prevents renal metabolism of Imipenem (Tiepenem) so that when Imipenem (Tiepenem) and Cilastatin (Tiepenem) sodium are given concomitantly, increased levels of Imipenem (Tiepenem) are achieved in the urine. The binding of Imipenem (Tiepenem) to human serum proteins is approximately 20% and that of Cilastatin (Tiepenem) is approximately 40%.

In a clinical study in which a 500-mg dose of the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium was administered to healthy subjects, the average peak level of Imipenem (Tiepenem) in interstitial fluid (skin blister fluid) was approximately 5.0 µg/mL within 3.5 hours after administration.

Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium is hemodialyzable. However, usefulness of this procedure in the overdosage setting is questionable.

Microbiology

The bactericidal activity of Imipenem (Tiepenem) results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin-binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B.

Imipenem (Tiepenem) has a high degree of stability in the presence of beta-lactamases, including penicillinases and cephalosporinases produced by gram-negative and gram-positive bacteria. It is a potent inhibitor of beta-lactamases from certain gram-negative bacteria which are inherently resistant to many beta-lactam antibiotics, e.g., Pseudomonas aeruginosa, Serratia spp. and Enterobacter spp.

Imipenem (Tiepenem) has in vitro activity against a wide range of gram-positive and gram-negative organisms. Imipenem (Tiepenem) has been shown to be active against most strains of the following microorganisms both in vitro and in clinical infections treated with the intramuscular formulation of Imipenem (Tiepenem)-Cilastatin (Tiepenem) sodium as described in the INDICATIONS section.

Gram-positive aerobes:

Staphylococcus aureus including penicillinase-producing strains

(NOTE: Methicillin-resistant staphylococci should be reported as resistant to Imipenem (Tiepenem).)

Group D streptococcus including Enterococcus faecalis (formerly S. faecalis)

(NOTE: Imipenem (Tiepenem) is inactive in vitro against Enterococcus faecium [formerly S. faecium].)

Streptococcus pneumoniae

Streptococcus pyogenes (Group A streptococci)

Streptococcus viridans group

Gram-negative aerobes:

Acinetobacter spp., including A. calcoaceticus

Citrobacter spp.

Enterobacter cloacae

Escherichia coli

Haemophilus influenzae

Klebsiella pneumoniae

Pseudomonas aeruginosa

(NOTE: Imipenem (Tiepenem) is inactive in vitro against Xanthomonas (Pseudomonas) maltophilia and P. cepacia.)

Gram-positive anaerobes:

Peptostreptococcus spp.

Gram-negative anaerobes:

Bacteroides spp., including

Bacteroides distasonis

Bacteroides intermedius (formerly B. melaninogenicus intermedius)

Bacteroides fragilis

Bacteroides thetaiotaomicron

Fusobacterium spp.

Imipenem (Tiepenem) exhibits in vitro minimal inhibitory concentrations (MICs) of 4 µg/mL or less against most ( ≥ 90%) strains of the following microorganisms; however, the safety and effectiveness of Imipenem (Tiepenem) in treating clinical infections due to these microorganisms have not been established in adequate and well-controlled clinical trials.

Gram-positive aerobes:

Bacillus spp.

Listeria monocytogenes

Nocardia spp.

Group C streptococci

Group G streptococci

Gram-negative aerobes:

Aeromonas hydrophila

Alcaligenes spp.

Capnocytophaga spp.

Enterobacter agglomerans

Haemophilus ducreyi

Klebsiella oxytoca

Neisseria gonorrhoeae including penicillinase-producing strains

Pasteurella spp.

Proteus mirabilis

Providencia stuartii

Gram-positive anaerobes:

Clostridium perfringens

Gram-negative anaerobes:

Prevotella bivia

Prevotella disiens

Prevotella melaninogenica

Veillonella spp.

In vitro tests show Imipenem (Tiepenem) to act synergistically with aminoglycoside antibiotics against some isolates of Pseudomonas aeruginosa.

Susceptibility Tests

Dilution techniques:

Use a standardized dilution method.

The MIC values obtained should be interpreted according to the following criteria:

MIC (µg/mL) Interpretation
≥ 4 Susceptible
8 Moderately Susceptible
≤ 16 Resistant

REFERENCES

1. National Committee for Clinical Laboratory Standards, Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that Grow Aerobically - Fourth Edition. Approved Standard NCCLS Document M7-A4, Vol. 17, No. 2 NCCLS, Villanova, PA, 1997.

2. National Committee for Clinical Laboratory Standards, Performance Standards for Antimicrobial Disk Susceptibility Tests - Sixth Edition. Approved Standard NCCLS Document M2-A6, Vol. 17, No. 1 NCCLS, Villanova, PA, 1997.

3. National Committee for Clinical Laboratory Standards, Method for Antimicrobial Susceptibility Testing of Anaerobic Bacteria - Third Edition. Approved Standard NCCLS Document M11-A3, Vol. 13, No. 26 NCCLS, Villanova, PA, 1993.



References

  1. DailyMed. "CILASTATIN SODIUM; IMIPENEM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. DailyMed. "CILASTATIN SODIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  3. NCIt. "Imipenem: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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