4-Aminopyridine Hydrochloride (Pymadin)

Paskov, D; Ágoston, S.; Bowman, W. C.

doi:10.1007/978-3-642-70682-0_33

Cited by 13 publications

(14 citation statements)

References 167 publications

(186 reference statements)

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“…K + channel blockade by 4-AP has other important physiological consequences with clinical relevance. Prolonged action current results in a larger than normal Ca 2+ influx at presynaptic terminals (70). This results in increased transmitter release from end terminals and enhanced neuro-neuronal or neuromuscular transmission (52,61,67), Kim et al (52,53), for example, showed that 4-AP produced dose-dependent increases in end plate potential amplitude, in rise time to peak, and in the average number of acetylcholine quanta released by nerve terminals.…”

Section: -Aminopyridine (Fampridine) 297mentioning

confidence: 99%

“…The principal mechanism of action of 4-AP is a dose-dependent block of fast, voltagegated K + channels (A current) in excitable membranes (70) and in nonexcitable cells such as B cells (122) or T lymphocytes (46). There are several different types of voltage-gated K + currents and channels in mammalian and human axons (80) and they exhibit varying degrees of sensitivity to 4-AP blockade.…”

Section: Pharmacology Of 4-apmentioning

confidence: 99%

“…For the purposes of this report, the term 4-AP or 4-aminopyridine is used to denote the compound in its various IR formulations, in order to distinguish it from fampridine-SR. There have been several previous reviews of 4-AP detailing its historical development, pharmacological properties and early clinical applications (70,98), including SCI (40) and MS (7,97). Since these were published there have been an appreciable number of new clinical trials.…”

Section: Introductionmentioning

confidence: 99%

“…1). The pyridine nitrogen of 4-AP has a pK a value of 9.1 so that at body pH about 98% of the molecules are protonated to form the monocation (70). The charge on the ionic form is delocalized over both nitrogens and this effectively prevents the addition of a second proton.…”

Section: Introductionmentioning

confidence: 99%

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The Use of 4‐Aminopyridine (Fampridine) in Demyelinating Disorders

Hayes¹

2004

CNS Drug Reviews

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4-Aminopyridine (4-AP or fampridine) is a potassium channel-blocking agent that has been shown to restore conduction in focally demyelinated axons. A sustained-release matrix tablet form of 4-AP (fampridine-SR) is currently undergoing multicenter clinical trials in patients with multiple sclerosis or chronic spinal cord injury. This review describes the pharmacology and mechanisms of action of 4-AP, its pharmacokinetics in human subjects, and the outcomes of clinical trials employing either immediate-release or sustained-release formulations of the drug. The randomized clinical trials that have been completed to date indicate that K+ channel blockade may prove to be a useful strategy for ameliorating central conduction deficits due to demyelination. Diverse neurological gains have been reported for both motor and sensory domains. At the present time, however, the clinical trials have not provided sufficiently robust or definitive evidence of efficacy to gain regulatory approval for the symptomatic management of patients with either multiple sclerosis or spinal cord injury.

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Section: -Aminopyridine (Fampridine) 297mentioning

confidence: 99%

Section: Pharmacology Of 4-apmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The Use of 4‐Aminopyridine (Fampridine) in Demyelinating Disorders

Hayes¹

2004

CNS Drug Reviews

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“…4-aminopyridine is a drug which acts by this mechanism. Its clinical usefulness is limited by virtue of its ability to enter the central nervous system, thereby giving rise to convulsions (5).…”

Section: Contraindicationsmentioning

confidence: 99%