Fampridine 10mg capsules
Requires a prescription from a doctor or prescriber
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
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Official medicine documents
Safety monitoring data
Yellow Card reports
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Suspected adverse reactions reported for Fampridine
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Fampridine
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Fampridine
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & product information
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
3.5 hours
Mechanism
In MS, axons are progressively demyelinated which exposes potassium channels.
Food interactions
1 warning
Human targets
16 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1 hour
Half-life
3.5 hours
Extended release form = 5.47 hours;
Protein binding
10 mg
Volume of distribution
10 mg
Metabolism
Elimination
24 hours
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 864 interactions
LD50, oral, rat = 21 mg/kg
Dalfampridine inhibits voltage-gated potassium channels in the CNS to maintain the transmembrane potential and prolong action potential. In other words, dalfampridine works to make sure that the current available is high enough to stimulate conduction in demyelinated axons that are exposed in MS patients. Furthermore, it facilitates neuromuscular and synaptic transmission by relieving conduction blocks in demyelinated axons.
How the body processes this drug — absorption, distribution, metabolism, and elimination
Tmax, immediate release form = 1 hour;
Tmax, extended release form = 3.5 hours;
Cmax, 10 mg extended release = 17.3 - 21.6 ng/mL;
Relative bioavailability of 10 mg extended-release tablets compared to aqueous oral solution = 96%
Extended release form = 5.47 hours;
Urine (96%; 90% of total dose as unchanged drug);
Feces (0.5%)
Proteins and enzymes this drug interacts with in the body
PMID:19903818 PMID:8845167
Contributes to the regulation of the membrane potential and nerve signaling, and prevents neuronal hyperexcitability .
PMID:17156368
Forms tetrameric potassium-selective channels through which potassium ions pass in accordance with their electrochemical gradient. The channel alternates between opened and closed conformations in response to the voltage difference across the membrane .
PMID:19912772
Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, KCNA6, KCNA7, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel .
PMID:12077175 PMID:17156368
Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation of delayed rectifier potassium channels .
PMID:12077175 PMID:17156368
In vivo, membranes probably contain a mixture of heteromeric potassium channel complexes, making it difficult to assign currents observed in intact tissues to any particular potassium channel family member. Homotetrameric KCNA1 forms a delayed-rectifier potassium channel that opens in response to membrane depolarization, followed by slow spontaneous channel closure .
PMID:19307729 PMID:19903818 PMID:19912772 PMID:19968958
In contrast, a heterotetrameric channel formed by KCNA1 and KCNA4 shows rapid inactivation .
PMID:17156368
Regulates neuronal excitability in hippocampus, especially in mossy fibers and medial perforant path axons, preventing neuronal hyperexcitability.
Response to toxins that are selective for KCNA1, respectively for KCNA2, suggests that heteromeric potassium channels composed of both KCNA1 and KCNA2 play a role in pacemaking and regulate the output of deep cerebellar nuclear neurons (By similarity). May function as down-stream effector for G protein-coupled receptors and inhibit GABAergic inputs to basolateral amygdala neurons (By similarity). May contribute to the regulation of neurotransmitter release, such as gamma-aminobutyric acid (GABA) release (By similarity).
Plays a role in regulating the generation of action potentials and preventing hyperexcitability in myelinated axons of the vagus nerve, and thereby contributes to the regulation of heart contraction (By similarity). Required for normal neuromuscular responses .
PMID:11026449 PMID:17136396
Regulates the frequency of neuronal action potential firing in response to mechanical stimuli, and plays a role in the perception of pain caused by mechanical stimuli, but does not play a role in the perception of pain due to heat stimuli (By similarity). Required for normal responses to auditory stimuli and precise location of sound sources, but not for sound perception (By similarity).
The use of toxins that block specific channels suggest that it contributes to the regulation of the axonal release of the neurotransmitter dopamine (By similarity). Required for normal postnatal brain development and normal proliferation of neuronal precursor cells in the brain (By similarity). Plays a role in the reabsorption of Mg(2+) in the distal convoluted tubules in the kidney and in magnesium ion homeostasis, probably via its effect on the membrane potential PMID:19307729 PMID:23903368
The channel alternates between opened and closed conformations in response to the voltage difference across the membrane .
PMID:11211111 PMID:19912772 PMID:23769686 PMID:8495559
Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, KCNA6, KCNA7, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel .
PMID:20220134 PMID:8495559
Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation of delayed rectifier potassium channels. In vivo, membranes probably contain a mixture of heteromeric potassium channel complexes, making it difficult to assign currents observed in intact tissues to any particular potassium channel family member. Homotetrameric KCNA2 forms a delayed-rectifier potassium channel that opens in response to membrane depolarization, followed by slow spontaneous channel closure .
PMID:19912772 PMID:23769686
In contrast, a heteromultimer formed by KCNA2 and KCNA4 shows rapid inactivation .
PMID:8495559
Regulates neuronal excitability and plays a role as pacemaker in the regulation of neuronal action potentials (By similarity).
KCNA2-containing channels play a presynaptic role and prevent hyperexcitability and aberrant action potential firing (By similarity). Response to toxins that are selective for KCNA2-containing potassium channels suggests that in Purkinje cells, dendritic subthreshold KCNA2-containing potassium channels prevent random spontaneous calcium spikes, suppressing dendritic hyperexcitability without hindering the generation of somatic action potentials, and thereby play an important role in motor coordination (By similarity). Plays a role in the induction of long-term potentiation of neuron excitability in the CA3 layer of the hippocampus (By similarity).
May function as down-stream effector for G protein-coupled receptors and inhibit GABAergic inputs to basolateral amygdala neurons (By similarity). May contribute to the regulation of neurotransmitter release, such as gamma-aminobutyric acid (GABA) (By similarity). Contributes to the regulation of the axonal release of the neurotransmitter dopamine (By similarity).
Reduced KCNA2 expression plays a role in the perception of neuropathic pain after peripheral nerve injury, but not acute pain (By similarity). Plays a role in the regulation of the time spent in non-rapid eye movement (NREM) sleep (By similarity)
PMID:19912772 PMID:8495559
Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel .
PMID:8495559
Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation.
In vivo, membranes probably contain a mixture of heteromeric potassium channel complexes, making it difficult to assign currents observed in intact tissues to any particular potassium channel family member. Homotetrameric KCNA4 forms a potassium channel that opens in response to membrane depolarization, followed by rapid spontaneous channel closure .
PMID:19912772 PMID:8495559
Likewise, a heterotetrameric channel formed by KCNA1 and KCNA4 shows rapid inactivation PMID:17156368
Can form functional homotetrameric channels and heterotetrameric channels that contain variable proportions of KCNA1, KCNA2, KCNA4, KCNA5, and possibly other family members as well; channel properties depend on the type of alpha subunits that are part of the channel .
PMID:12130714
Channel properties are modulated by cytoplasmic beta subunits that regulate the subcellular location of the alpha subunits and promote rapid inactivation .
PMID:12130714
Homotetrameric channels display rapid activation and slow inactivation .
PMID:12130714 PMID:8505626
Required for normal electrical conduction including formation of the infranodal ventricular conduction system and normal action potential configuration, as a result of its interaction with XIRP2 (By similarity). May play a role in regulating the secretion of insulin in normal pancreatic islets
Enzymes involved in drug metabolism — important for understanding drug interactions
Proteins that transport this drug across cell membranes
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID:9687576
However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow .
PMID:15783073
Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters .
PMID:16581093 PMID:17460754 PMID:9687576
Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system .
PMID:17460754
Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
ATC N07XX07
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Dalfampridine
Matched from: Fampridine
Additional database identifiers
Drugs Product Database (DPD)
21173
ChemSpider
1664
BindingDB
10458
ZINC
ZINC000000599985
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6218
GenAtlas
KCNA1
GeneCards
KCNA1
GenBank Gene Database
L02750
GenBank Protein Database
186663
Guide to Pharmacology
538
UniProt Accession
KCNA1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6220
GeneCards
KCNA2
Guide to Pharmacology
539
UniProt Accession
KCNA2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6221
GeneCards
KCNA3
Guide to Pharmacology
540
UniProt Accession
KCNA3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6222
GeneCards
KCNA4
UniProt Accession
KCNA4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6224
GeneCards
KCNA5
Guide to Pharmacology
542
UniProt Accession
KCNA5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6225
GeneCards
KCNA6
Guide to Pharmacology
543
UniProt Accession
KCNA6_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6226
GeneCards
KCNA7
Guide to Pharmacology
544
UniProt Accession
KCNA7_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6219
GeneCards
KCNA10
Guide to Pharmacology
545
UniProt Accession
KCA10_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6231
GeneCards
KCNB1
Guide to Pharmacology
546
UniProt Accession
KCNB1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6232
GeneCards
KCNB2
Guide to Pharmacology
547
UniProt Accession
KCNB2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6233
GeneCards
KCNC1
UniProt Accession
KCNC1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6234
GeneCards
KCNC2
Guide to Pharmacology
549
UniProt Accession
KCNC2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6235
GeneCards
KCNC3
UniProt Accession
KCNC3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6237
GeneCards
KCND1
Guide to Pharmacology
552
UniProt Accession
KCND1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6238
GeneCards
KCND2
GenBank Gene Database
AF121104
GenBank Protein Database
4530478
UniProt Accession
KCND2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6239
GeneCards
KCND3
GenBank Gene Database
AF048712
GenBank Protein Database
2935434
UniProt Accession
KCND3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2631
GeneCards
CYP2E1
GenBank Gene Database
J02625
GenBank Protein Database
181360
Guide to Pharmacology
1330
UniProt Accession
CP2E1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10966
GeneCards
SLC22A2
GenBank Gene Database
X98333
GenBank Protein Database
2281942
Guide to Pharmacology
1020
UniProt Accession
S22A2_HUMAN
Patent information
2 active patents, 4 expired
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: