Details of the Drug

General Information of Drug (ID: DMDVP3B)

• Drug Name: Pregabalin
• Synonyms: Pregabalin CR; Pregabalin (controlled-release, oral); Pregabalin (controlled-release, oral), Pfizer

Indication

Disease Entry	ICD 11	Status	REF
Chronic obstructive pulmonary disease	CA22	Approved	[1]
Epilepsy	8A60-8A68	Approved	[2]
Pain	MG30-MG3Z	Approved	[2]
Postherpetic neuralgia	1E91.5	Approved	[2]
Vulvodynia	N.A.	Approved	[2]
Chronic pain	MG30	Investigative	[2]
Neuralgia	N.A.	Investigative	[2]

• Affected Organisms: Humans and other mammals
• ATC Code:
  N02BF02: Pregabalin
  N02BF: Gabapentinoids
  N02B: OTHER ANALGESICS AND ANTIPYRETICS
  N02: ANALGESICS
  N: NERVOUS SYSTEM
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 159.23
  Logarithm of the Partition Coefficient (xlogp); -1.6
  Rotatable Bond Count (rotbonds); 5
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 3
• ADMET Property:
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 1.5 h [3]
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
  Bioavailability: The bioavailability of drug is over 90% [3]
  Clearance: The renal clearance of drug is 67.0-80.9 mL/min [5]
  Elimination: 90% of drug is excreted from urine in the unchanged form [4]
  Half-life: The concentration or amount of drug in body reduced by one-half in 6.3 hours [5]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 53.83 micromolar/kg/day [6]
  Vd: The volume of distribution (Vd) of drug is 0.5 L/kg [5]
  Water Solubility: The ability of drug to dissolve in water is measured as 33 mg/mL [4]
• Chemical Identifiers:
  Formula: C8H17NO2
  IUPAC Name: (3S)-3-(aminomethyl)-5-methylhexanoic acid
  Canonical SMILES: CC(C)C[C@@H](CC(=O)O)CN
  InChI: InChI=1S/C8H17NO2/c1-6(2)3-7(5-9)4-8(10)11/h6-7H,3-5,9H2,1-2H3,(H,10,11)/t7-/m0/s1
  InChIKey: AYXYPKUFHZROOJ-ZETCQYMHSA-N
• Cross-matching ID:
  PubChem CID: 5486971
  ChEBI ID: CHEBI:64356
  CAS Number: 148553-50-8
  UNII: 55JG375S6M
  DrugBank ID: DB00230
  TTD ID: D00WUF
  VARIDT ID: DR01255
  ACDINA ID: D00553
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1)	TTFK1JQ	CA2D1_HUMAN	Modulator	[7]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
L-type amino acid transporter 1 (SLC7A5)	DT48T0N	LAT1_HUMAN	Substrate	[8]

Molecular Expression Atlas of This Drug

• ICD Disease Classification: 12 Disease of the respiratory system
• Disease Class: ICD-11: CA23 Asthma
• The Studied Tissue: Lung tissue
• The Studied Disease: Chronic obstructive pulmonary disease [ICD-11:CA23]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1)	DTT	CACNA2D1	9.36E-01	-0.03	-0.13
Voltage-gated calcium channel alpha-2/delta-1 (CACNA2D1)	DTT	CACNA2D1	2.81E-05	-0.15	-0.68
L-type amino acid transporter 1 (SLC7A5)	DTP	LAT1	8.50E-01	1.70E-01	1.79E-01
L-type amino acid transporter 1 (SLC7A5)	DTP	LAT1	2.96E-04	3.30E-01	8.32E-01

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Pregabalin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Pregabalin and Oliceridine.	Acute pain [MG31]	[9]
Dihydrocodeine	DMB0FWL	Major	Additive CNS depression effects by the combination of Pregabalin and Dihydrocodeine.	Chronic pain [MG30]	[10]
Morphine	DMRMS0L	Major	Additive CNS depression effects by the combination of Pregabalin and Morphine.	Chronic pain [MG30]	[9]
Levomilnacipran	DMV26S8	Moderate	Antagonize the effect of Pregabalin when combined with Levomilnacipran.	Chronic pain [MG30]	[11]
Olopatadine	DMKMWQG	Moderate	Additive CNS depression effects by the combination of Pregabalin and Olopatadine.	Conjunctiva disorder [9A60]	[12]
Remifentanil	DMZTXCH	Major	Additive CNS depression effects by the combination of Pregabalin and Remifentanil.	Corneal disease [9A76-9A78]	[9]
Methadone	DMTW6IU	Major	Additive CNS depression effects by the combination of Pregabalin and Methadone.	Cough [MD12]	[9]
Ethanol	DMDRQZU	Moderate	Additive CNS depression effects by the combination of Pregabalin and Ethanol.	Cystitis [GC00]	[12]
Sertraline	DM0FB1J	Moderate	Antagonize the effect of Pregabalin when combined with Sertraline.	Depression [6A70-6A7Z]	[11]
Fluoxetine	DM3PD2C	Moderate	Antagonize the effect of Pregabalin when combined with Fluoxetine.	Depression [6A70-6A7Z]	[11]
Vilazodone	DM4LECQ	Moderate	Antagonize the effect of Pregabalin when combined with Vilazodone.	Depression [6A70-6A7Z]	[11]
Paroxetine	DM5PVQE	Moderate	Antagonize the effect of Pregabalin when combined with Paroxetine.	Depression [6A70-6A7Z]	[11]
Vortioxetine	DM6F1PU	Moderate	Antagonize the effect of Pregabalin when combined with Vortioxetine.	Depression [6A70-6A7Z]	[11]
Duloxetine	DM9BI7M	Moderate	Antagonize the effect of Pregabalin when combined with Duloxetine.	Depression [6A70-6A7Z]	[11]
Milnacipran	DMBFE74	Moderate	Antagonize the effect of Pregabalin when combined with Milnacipran.	Depression [6A70-6A7Z]	[11]
Escitalopram	DMFK9HG	Moderate	Antagonize the effect of Pregabalin when combined with Escitalopram.	Depression [6A70-6A7Z]	[11]
Desvenlafaxine	DMHD4PE	Moderate	Antagonize the effect of Pregabalin when combined with Desvenlafaxine.	Depression [6A70-6A7Z]	[11]
Venlafaxine	DMR6QH0	Moderate	Antagonize the effect of Pregabalin when combined with Venlafaxine.	Depression [6A70-6A7Z]	[11]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Pregabalin and Esketamine.	Depression [6A70-6A7Z]	[13]
Brimonidine	DMQLT4N	Moderate	Additive CNS depression effects by the combination of Pregabalin and Brimonidine.	Glaucoma [9C61]	[14]
Chloroquine	DMSI5CB	Moderate	Antagonize the effect of Pregabalin when combined with Chloroquine.	Malaria [1F40-1F45]	[13]
Hydroxychloroquine	DMSIVND	Moderate	Antagonize the effect of Pregabalin when combined with Hydroxychloroquine.	Malaria [1F40-1F45]	[13]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Pregabalin and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[15]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Pregabalin and Lasmiditan.	Migraine [8A80]	[16]
Flibanserin	DM70DTN	Moderate	Additive CNS depression effects by the combination of Pregabalin and Flibanserin.	Mood disorder [6A60-6E23]	[17]
Thalidomide	DM70BU5	Moderate	Additive CNS depression effects by the combination of Pregabalin and Thalidomide.	Multiple myeloma [2A83]	[18]
Levomethadyl Acetate	DM06HG5	Major	Additive CNS depression effects by the combination of Pregabalin and Levomethadyl Acetate.	Opioid use disorder [6C43]	[10]
Apraclonidine	DMO4PVE	Moderate	Additive CNS depression effects by the combination of Pregabalin and Apraclonidine.	Optic nerve disorder [9C40]	[14]
Pentazocine	DM1XBHS	Major	Additive CNS depression effects by the combination of Pregabalin and Pentazocine.	Pain [MG30-MG3Z]	[9]
Dextropropoxyphene	DM23HCX	Major	Additive CNS depression effects by the combination of Pregabalin and Dextropropoxyphene.	Pain [MG30-MG3Z]	[10]
Butorphanol	DM5KYPJ	Major	Additive CNS depression effects by the combination of Pregabalin and Butorphanol.	Pain [MG30-MG3Z]	[9]
Oxymorphone	DM65AGJ	Major	Additive CNS depression effects by the combination of Pregabalin and Oxymorphone.	Pain [MG30-MG3Z]	[9]
Levorphanol	DMGS80V	Major	Additive CNS depression effects by the combination of Pregabalin and Levorphanol.	Pain [MG30-MG3Z]	[9]
Hydromorphone	DMHP21E	Major	Additive CNS depression effects by the combination of Pregabalin and Hydromorphone.	Pain [MG30-MG3Z]	[9]
Dezocine	DMJDB0Y	Major	Additive CNS depression effects by the combination of Pregabalin and Dezocine.	Pain [MG30-MG3Z]	[9]
Codeine	DMJX6ZG	Major	Additive CNS depression effects by the combination of Pregabalin and Codeine.	Pain [MG30-MG3Z]	[9]
Nalbuphine	DMOSQGU	Major	Additive CNS depression effects by the combination of Pregabalin and Nalbuphine.	Pain [MG30-MG3Z]	[9]
Buprenorphine	DMPRI8G	Major	Additive CNS depression effects by the combination of Pregabalin and Buprenorphine.	Pain [MG30-MG3Z]	[19]
Hydrocodone	DMQ2JO5	Major	Additive CNS depression effects by the combination of Pregabalin and Hydrocodone.	Pain [MG30-MG3Z]	[9]
Meperidine	DMX4GND	Major	Additive CNS depression effects by the combination of Pregabalin and Meperidine.	Pain [MG30-MG3Z]	[9]
Oxycodone	DMXLKHV	Major	Additive CNS depression effects by the combination of Pregabalin and Oxycodone.	Pain [MG30-MG3Z]	[9]
Fentanyl	DM8WAHT	Major	Additive CNS depression effects by the combination of Pregabalin and Fentanyl.	Sensation disturbance [MB40]	[9]
Sufentanil	DMU7YEL	Major	Additive CNS depression effects by the combination of Pregabalin and Sufentanil.	Sensation disturbance [MB40]	[9]
Tizanidine	DMR2IQ4	Moderate	Additive CNS depression effects by the combination of Pregabalin and Tizanidine.	Tonus and reflex abnormality [MB47]	[20]
Cetirizine	DMOMP9U	Moderate	Additive CNS depression effects by the combination of Pregabalin and Cetirizine.	Vasomotor/allergic rhinitis [CA08]	[21]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Eisenoxyd	E00585	56841934	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Potassium hydroxide	E00233	14797	Alkalizing agent
Propylene glycol	E00040	1030	Antimicrobial preservative; Humectant; Plasticizing agent; Solvent
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Pregabalin 225 mg capsule	225 mg	Oral Capsule	Oral
Pregabalin 300 mg capsule	300 mg	Oral Capsule	Oral
Pregabalin 150 mg capsule	150 mg	Oral Capsule	Oral
Pregabalin 25 mg capsule	25 mg	Oral Capsule	Oral
Pregabalin 50 mg capsule	50 mg	Oral Capsule	Oral
Pregabalin 75 mg capsule	75 mg	Oral Capsule	Oral
Pregabalin 100 mg capsule	100 mg	Oral Capsule	Oral
Pregabalin 200 mg capsule	200 mg	Oral Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5484).
• [2] Pregabalin FDA Label
• [3] Ben-Menachem E: Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8.
• [4] BDDCS applied to over 900 drugs
• [5] FDA Label Pregabalin
• [6] Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
• [7] Pregabalin reduces the release of synaptic vesicles from cultured hippocampal neurons. Mol Pharmacol. 2006 Aug;70(2):467-76.
• [8] Transport of Pregabalin Via L-Type Amino Acid Transporter 1 (SLC7A5) in Human Brain Capillary Endothelial Cell Line. Pharm Res. 2018 Oct 29;35(12):246.
• [9] Eckhardt K, Ammon S, Hofmann U, Riebe A, Gugeler N, Mikus G "Gabapentin enhances the analgesic effect of morphine in healthy volunteers." Anesth Analg 91 (2000): 185-91. [PMID: 10866910]
• [10] Eipe N, Penning J "Postoperative respiratory depression associated with pregabalin: a case series and a preoperative decision algorithm." Pain Res Manag 16 (2011): 353-6. [PMID: 22059207]
• [11] Belcastro V, Costa C, Striano P "Levetiracetam-associated hyponatremia." Seizure 17 (2008): 389-90. [PMID: 18584781]
• [12] Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002]
• [13] Cerner Multum, Inc. "Australian Product Information.".
• [14] Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA.
• [15] Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
• [16] Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
• [17] Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC.
• [18] Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ.
• [19] Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200]
• [20] Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY.
• [21] Product Information. Zyrtec (cetirizine). Pfizer US Pharmaceuticals, New York, NY.