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what to do if piracetam makes you tired

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Piracetam

Summary

Piracetam is a nootropic cyclic GABA derivative used in myoclonus, sickle cell illness, alcohol dependence, and equally a general cognitive enhancer.

Generic Name
Piracetam
DrugBank Accession Number
DB09210
Groundwork

Piracetam is a nootropic drug in the racetams group, with chemical proper name 2-oxo-1-pyrrolidine acetamide. It shares the same two-oxo-pyrrolidone base construction with pyroglutamic acid and is a cyclic derivative of the neurotransmitter γ-aminobutyric acid (GABA). All the same its mechanism of activeness differ from that of endogenous GABA. Piracetam has neuroprotective and anticonvulsant properties and is reported to improve neural plasticity ane. Its efficacy is documented in cognitive disorders and dementia, vertigo, cortical myoclonus, dyslexia, and sickle cell anemia although the clinical awarding in these conditions is not yet established. Piracetam has effects on the vascular system by reducing erythrocyte adhesion to the vascular endothelium, hindering vasospasms and facilitating microcirculation one.

Originally marketed by UCB Pharma in 1971, piracetam was the offset nootropic drug to attune cerebral office without causing sedation or stimulation ane. It is not approved for any medical or dietary use past the FDA. In the U.k., piracetam is prescribed mainly for myoclonus, but is used off-label for other conditions such every bit learning difficulties in children, retentivity loss or other cerebral defects in the elderly, and sickle-cell vaso-occlusive crises iv. Evidence to support its use for many conditions is unclear.

Type
Pocket-sized Molecule
Groups
Approved, Investigational
Structure

Weight
Average: 142.1558
Monoisotopic: 142.074227574
Chemic Formula
C6HtenN2O2
Synonyms
  • Piracetam
  • Piracetamum
External IDs
  • CL-871
  • KT-801
  • UCB 6215
Indication

Indicated in adult patients suffering from myoclonus of cortical origin, irrespective of aetiology, and should be used in combination with other anti-myoclonic therapies 5.

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Associated Weather
  • Alcohol Dependency
  • Alcohol Withdrawal Syndrome
  • Cognitive Deficits caused past Injuries, Craniocerebral
  • Cerebral Dysfunctions
  • Cognitive Impairment (CI)
  • Comatose acquired by Blood Vessel (Vascular) Dysfunction
  • Comatose caused past CNS Toxicity
  • Comatose caused by Traumas
  • Learning Disorders
  • Myoclonus
  • Sickle Jail cell Affliction (SCD)
  • Giddiness caused by Injuries, Craniocerebral
Contraindications & Blackbox Warnings

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Pharmacodynamics

Piracetam is known to mediate various pharmacodynamic deportment:

Neuronal effects:

Piracetam modulates the cholinergic, serotonergic, noradrenergic, and glutamatergic neurotransmission although the drug does not display high affinity to any of the associated receptors (Ki >10μM). Instead, piracetam increases the density of postsynaptic receptors and/or restore the function of these receptors through stabilizing the membrane fluidity 1. In the forebrain of crumbling mice, the density of NMDA receptors was increased by approximately twenty% post-obit 14 days of piracetam handling. Based on the findings of various animal and human studies, the cerebral processses including learning, retention, attention and consciousness were enhanced from piracetam therapy without inducing sedation and psychostimulant effects 5. Piracetam mediate neuroprotective effects against hypoxia-induced damage, intoxication, and electroconvulsive therapy five.

In ii studies involving alcohol-treated rats with evidences of withdrawal-related neuronal loss, piracetam was shown to reduce the extent of neuronal loss and increase the numbers of synapses in the hippocampus by up to 20% relative to alcohol-treated or alcohol-withdrawn rats one. This suggests that piracetam is capable in promoting neuroplasticity when recoverable neural circuits are present 1. Although the mechanism of activeness is not fully understood, administration of piracetam prior to a convulsant stimulus reduces the seizure severity and enhances the anticonvulsant effectiveness of conventional antiepileptics such every bit carbamazepine and diazepam three.

Vascular effects:

Piracetam is shown to increase the deformability of erythrocytes, reduce platelet aggregation in a dose-dependent manner, reduce the adhesion of erythrocytes to vascular endothelium and capillary vasospasm. In healthy volunteers, piracetam mediated a straight stimulant effect on prostacycline synthesis and reduced the plasma levels of fibrinogen and von Willebrand'southward factors (VIII: C; 8 R: AG; Eight R: vW) by 30 to twoscore% v. Potentiated microcirculation is thought to arise from a combination of effects on erythrocytes, claret vessels and claret coagulation one.

Machinery of action

Piracetam interacts with the polar heads in the phospholipids membrane and the resulting mobile drug-lipid complexes are thought to reorganize the lipids and influence membrane part and fluidity 1. Such interaction has been reported in a study that investigated the effects of neuronal outgrowth induced past beta amyloid peptides; while amyloid peptides cause lipid disorganization within the jail cell membranes leading to neuronal decease, piracetam demonstrated to decrease the destabilizing effects of amyloid peptide ii. The authors suggest that piracetam induces a positive curvature of the membrane by occupying the polar groups in the phospholipids to annul the negative curvature induced past amyloid peptides , which in plough would subtract the likelihood of membrane fusion 1. This mechanism of activeness is thought to ameliorate membrane stability, allowing the membrane and transmembrane proteins to maintain and recover the three-dimensional structure or folding for normal function 4 such as membrane transport, chemic secretion, and receptor binding and stimulation i.

Through restored membrane fluidity, piracetam promotes restored neurotransmission such as glutamatergic and cholinergic systems, enhances neuroplasticity and mediates neuroprotective and anticonvulsant effects at the neuronal level 1. It is also demonstrated that piracetam also improves the fluidity of platelet membranes. At the vascular level, piracetam decreases adhesion of erythrocytes to jail cell wall and reduces vasospasm which in turn improves microcirculation including cerebral and renal blood flow 1.

Absorption

Piracetam displays a linear and fourth dimension-dependent pharmacokinetic backdrop with low intersubject variability over a big range of doses. Piracetam is apace and extensively absorbed following oral administration with the top plasma concentration is reached within 1 hour after dosing in fasted subjects. Following a unmarried oral dose of 3.2 grand piracetam, the peak plasma concentration (Cmax) was 84 µg/mL. Intake of food may decrease the Cmax by 17% and increase the time to accomplish Cmax (Tmax) from one to 1.5 hours. Tmax in the cerebrospinal fluid is accomplished approximately 5 hours post-assistants four.

The absolute bioavailability of piracetam oral formulations is shut to 100% and the steady state plasma concentrations are achieved inside iii days of dosing four.

Volume of distribution

Vd is approximately 0.6L/kg. Piracetam may cross the blood-brain bulwark as it was measured in the cerebrospinal fluid following intravenous administration iv. Piracetam diffuses to all tissues except adipose tissues, crosses placental barrier and penetrates the membranes of isolated red blood cells 4.

Protein binding

Piracetam is not reported to be bound to plasma proteins 4.

Metabolism

As large proportion of total piracetam administered is excreted equally unchanged drug, there is no known major metabolism of piracetam 4.

Route of elimination

Piracetam is predominantly excreted via renal emptying, where about 80-100% of the full dose is recovered in the urine. Approximately 90% of the dose of piracetam is excreted in the urine as unchanged drug 4.

Half-life

The plasma half life of piracetam is approximately 5 hours following oral or intravenous assistants. The half life in the cerebrospinal fluid was 8.5 hours 4.

Clearance

The apparent total body clearance is lxxx-90 mL/min four.

Adverse Effects

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Toxicity

The cases of overdose with piracetam is rare. The highest reported overdose with piracetam was oral intake of 75g which was associated with diarrhea and abdominal pain; the signs were most likely related to the extreme high dose of sorbitol contained in the used formulation. In cases of acute, meaning overdosage, stomach emptying by gastric lavage or induced emesis is recommended equally there are no known antidotes for piracetam 4. Direction for an overdose will well-nigh likely be symptomatic treatment and may include hemodialysis, where the extraction efficacy of the dialyser is 50 to sixty% for the drug 4.

Oral LD50 in a mouse acute toxicity study was 2000 mg/kg MSDS.

Pathways
Non Bachelor
Pharmacogenomic Effects/ADRs
Not Bachelor
Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If y'all believe you are experiencing an interaction, contact a healthcare provider immediately. The absenteeism of an interaction does not necessarily mean no interactions exist.

  • Canonical
  • Vet canonical
  • Nutraceutical
  • Illicit
  • Withdrawn
  • Investigational
  • Experimental
  • All Drugs
Drug Interaction

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interactions in your software
Abacavir Abacavir may decrease the excretion rate of Piracetam which could result in a college serum level.
Aceclofenac Aceclofenac may subtract the excretion rate of Piracetam which could issue in a higher serum level.
Acemetacin Acemetacin may subtract the excretion rate of Piracetam which could result in a higher serum level.
Acetaminophen Acetaminophen may decrease the excretion rate of Piracetam which could upshot in a higher serum level.
Acetazolamide Acetazolamide may increment the excretion rate of Piracetam which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid Acetylsalicylic acid may subtract the excretion rate of Piracetam which could result in a higher serum level.
Aclidinium Aclidinium may decrease the excretion charge per unit of Piracetam which could event in a college serum level.
Acrivastine Piracetam may decrease the excretion charge per unit of Acrivastine which could result in a college serum level.
Acyclovir Acyclovir may decrease the excretion rate of Piracetam which could consequence in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Piracetam which could result in a higher serum level.
Nutrient Interactions
Not Available

Drug production information from 10+ global regions

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International/Other Brands
Myocalm (Taiho Pharmaceuticals)
ATC Codes
N06BX03 — Piracetam
  • N06BX — Other psychostimulants and nootropics
  • N06B — PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS
  • N06 — PSYCHOANALEPTICS
  • N — NERVOUS Organisation
Drug Categories
  • Acetamides
  • Acetates
  • Acids, Acyclic
  • Amides
  • Cardinal Nervous System Agents
  • Compounds used in a inquiry, industrial, or household setting
  • Drugs that are Mainly Renally Excreted
  • Nervous System
  • Neuroprotective Agents
  • Nootropic Agents
  • Protective Agents
  • Psychoanaleptics
  • Psychostimulants, Agents Used for ADHD and Nootropics
  • Pyrrolidines
  • Pyrrolidinones
Chemic TaxonomyProvided by Classyfire
Description
This chemical compound belongs to the grade of organic compounds known as blastoff amino acids and derivatives. These are amino acids in which the amino group is attached to the carbon atom immediately side by side to the carboxylate grouping (alpha carbon), or a derivative thereof.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Course
Amino acids, peptides, and analogues
Directly Parent
Alpha amino acids and derivatives
Culling Parents
Pyrrolidine-two-ones / North-alkylpyrrolidines / Third carboxylic acrid amides / Chief carboxylic acid amides / Lactams / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds evidence 1 more
Substituents
ii-pyrrolidone / Aliphatic heteromonocyclic compound / Blastoff-amino acrid or derivatives / Azacycle / Carbonyl group / Carboxamide group / Hydrocarbon derivative / Lactam / N-alkylpyrrolidine / Organic nitrogen chemical compound / Organic oxide / Organic oxygen compound / Organoheterocyclic chemical compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Primary carboxylic acid amide / Pyrrolidine / Pyrrolidone / Tertiary carboxylic acrid amide evidence 10 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
Not Available
Affected organisms
Not Bachelor
UNII
ZH516LNZ10
CAS number
7491-74-nine
InChI Key
GMZVRMREEHBGGF-UHFFFAOYSA-N
InChI

InChI=1S/C6H10N2O2/c7-5(9)4-8-3-1-2-6(8)ten/h1-4H2,(H2,7,9)

IUPAC Name

2-(ii-oxopyrrolidin-1-yl)acetamide

SMILES

NC(=O)CN1CCCC1=O

General References
  1. Winblad B: Piracetam: a review of pharmacological backdrop and clinical uses. CNS Drug Rev. 2005 Summer;11(2):169-82. [Commodity]
  2. Kurz C, Ungerer I, Lipka U, Kirr S, Schutt T, Eckert A, Leuner K, Muller Nosotros: The metabolic enhancer piracetam ameliorates the damage of mitochondrial role and neurite outgrowth induced by beta-amyloid peptide. Br J Pharmacol. 2010 May;160(ii):246-57. doi: 10.1111/j.1476-5381.2010.00656.x. Epub 2010 Mar 9. [Article]
  3. Fischer W, Kittner H, Regenthal R, Russo Eastward, De Sarro G: Furnishings of piracetam lone and in combination with antiepileptic drugs in rodent seizure models. J Neural Transm (Vienna). 2004 Sep;111(9):1121-39. doi: x.1007/s00702-004-0155-6. Epub 2004 May 14. [Article]
  4. Nootropil tablets Drug Summary [Link]
  5. electronic Medicines Compendium (eMC): Nootripil Summary of Product Characteristics [Link]
ChemSpider
4677
BindingDB
62877
RxNav
8351
ChEBI
32010
ChEMBL
CHEMBL36715
ZINC
ZINC000003812874
PDBe Ligand
PZI
Wikipedia
Piracetam
PDB Entries
3lsf / 3lsl / 3lsx
MSDS
Clinical Trials
Phase Status Purpose Conditions Count
4 Completed Treatment Vertigo, Peripheral 1
4 Terminated Treatment Acute Ischaemic Eye Cognitive Avenue Stroke 1
3 Completed Handling Tardive Dyskinesia (TD) ane
iii Terminated Treatment Anxiety Disorders / Dementia / Depression / Psychosomatic Disorders / Schizophrenia ane
3 Withdrawn Treatment Post-Poliomyelitis Syndrome 1
1 Completed Treatment Cocaine Related Disorders 1
ane Withdrawn Treatment Cocaine Related Disorders i
Not Bachelor Completed Not Available Alzheimer's Disease (AD) / Dementia / Vascular Dementia (VaD) 1
Not Bachelor Completed Treatment Memory Disorders one
Manufacturers

Not Available

Packagers

Non Available

Dosage Forms
Form Route Force
Injection Intravenous
Solution Intravenous
Tablet Oral
Solution / drops Oral
Injection Intravenous 200 MG/ML
Tablet, movie coated Oral
Pulverisation, for solution Oral
Solution 200 mg/1ml
Syrup Oral
Granule Oral
Syrup Oral 8 g
Tablet Oral 800 mg
Injection, solution Parenteral 3 G
Solution Parenteral 12 g/60ml
Injection, solution 12 Thousand/60ML
Solution Intravenous; Oral
Solution Intravenous; Oral 3 G/15ML
Solution Oral 20 %
Solution / drops Oral 33.33 %
Injection, solution Parenteral three m/15ml
Solution Conjunctival; Ophthalmic 0.two chiliad
Injection Parenteral 3 g
Syrup Oral 20 g
Solution Oral 20 chiliad/100ml
Pulverization Oral 48 g
Tablet, film coated Oral 1200.00 mg
Tablet, motion-picture show coated Oral 800.00 mg
Tablet, coated Oral 1200 mg
Injection Parenteral
Injection, solution Intravenous
Solution Oral
Injection, solution Intramuscular; Intravenous
Tablet Oral 1200 mg
Tablet, extended release Oral
Tablet, film coated Oral 800000 MG
Injection, solution
Injection, solution 3 1000/15ML
Solution Oral 333.three mg/ml
Solution Parenteral 1 thou/5ml
Solution Oral 33 %
Granule Oral 2.4 G
Tablet Oral 0.eight thou
Granule, for solution Oral
Granule, for suspension Oral
Injection
Injection Intramuscular; Intravenous
Capsule Oral
Tablet, coated Oral 800 mg
Capsule Oral 400 mg
Tablet, motion picture coated Oral 1200 mg
Tablet, moving-picture show coated Oral 800 mg
Prices
Not Bachelor
Patents
Not Available
Country
Solid
Experimental Properties
Property Value Source
melting point (°C) 152 MSDS
humid point (°C) Decomposes MSDS
Predicted Properties
Property Value Source
Water Solubility 479.0 mg/mL ALOGPS
logP -1.6 ALOGPS
logP -1.7 ChemAxon
logS 0.53 ALOGPS
pKa (Strongest Acidic) fifteen.93 ChemAxon
pKa (Strongest Basic) -ii ChemAxon
Physiological Charge 0 ChemAxon
Hydrogen Acceptor Count 2 ChemAxon
Hydrogen Donor Count 1 ChemAxon
Polar Surface Area 63.4 Å2 ChemAxon
Rotatable Bail Count 2 ChemAxon
Refractivity 35.06 grand3·mol-1 ChemAxon
Polarizability thirteen.96 Å3 ChemAxon
Number of Rings i ChemAxon
Bioavailability ane ChemAxon
Rule of 5 Yes ChemAxon
Ghose Filter No ChemAxon
Veber'due south Dominion No ChemAxon
MDDR-like Dominion No ChemAxon
Predicted ADMET Features
Not Available
Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Blazon Splash Cardinal
Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Non Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Non Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-002b-9400000000-651dc28016b653b55d23
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-002b-9400000000-9c47f9c6616fbfad2c93
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0002-9100000000-079c7eb43e2dcfe07d5f
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0002-9000000000-94d697783ea2c537498f
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-0002-9000000000-5dd797bddeacd8764c16
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-006t-9000000000-e270872ffd02b3d53ab2

Drug created at October 20, 2015 nineteen:46 / Updated at May 07, 2021 21:06

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Source: https://go.drugbank.com/drugs/DB09210

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