Lacosamide

Key takeaways

Lacosamide belongs to chemistry; place it in that map before memorising details.
Learn the definition first, then one example that makes the definition concrete.
Connect Lacosamide to a quantity you can measure, compute or draw — that is where exam questions come from.
Reproduce the core statement of Lacosamide from memory before moving on to harder problems.

Reference excerpt

Lacosamide, sold under the brand name Vimpat among others, is a medication used for the treatment of focal-onset seizures and primary generalized tonic–clonic seizures. It is used by mouth or intravenously. It is available as a generic medication.

Medical uses Lacosamide is indicated for the treatment of focal onset seizures and adjunctive therapy in the treatment of primary generalized tonic-clonic seizures.

Off-label use As with other anti-epileptic drugs (AEDs), lacosamide may have a variety of off-label uses, including for pain management and treatment of mental health disorders. Lacosamide and other AEDs have been used off-label in the management of bipolar disorder, cocaine addiction, dementia, depression, diabetic peripheral neuropathy, fibromyalgia, headache, hiccups, Huntington's disease, mania, migraine, obsessive-compulsive disorder, panic disorder, restless leg syndrome, and tinnitus. Combinations of AEDs are often employed for seizure reduction. Studies are underway for the use of lacosamide as a monotherapy for focal onset seizures, diabetic neuropathy, and fibromyalgia.

Contraindications The FDA has assigned lacosamide to pregnancy category C. Animal studies have reported incidences of fetal mortality and growth deficit. Lacosamide has not been tested during human pregnancy, and should be administered with caution. In addition, it has not been determined whether the excretion of lacosamide occurs in breast milk.

Side effects Lacosamide was generally well tolerated in adult patients with partial-onset seizures. The side-effects most commonly leading to discontinuation were dizziness, ataxia, diplopia (double vision), nystagmus, nausea, vertigo and drowsiness. These adverse reactions were observed in at least 10% of patients. Less common side-effects include tremors, blurred vision, vomiting and headache.

Gastrointestinal A generally well-tolerated drug, the most commonly reported gastrointestinal side effects of lacosamide are nausea, vomiting, and diarrhea.

Central nervous system Dizziness was the most common treatment-related adverse event. Other CNS effects are headache, drowsiness, blurred vision, involuntary movements, memory problems, diplopia (double vision), trembling or shaking of the hands, unsteadiness, ataxia.

Psychiatric Panic attacks; agitation or restlessness; irritability and aggression, anxiety, or depression; suicidality; insomnia and mania; altered mood; false and unusual sense of well-being. Lacosamide appears to have a low incidence of psychiatric side effects with psychosis reported in only 0.3% of patients.

Cardiovascular There is the risk of postural hypotension as well as arrhythmias. In addition, there is the possibility of atrioventricular block. There have also been post-marketing reports of lacosamide causing atrial fibrillation and atrial flutter in some populations, namely those with diabetic neuropathy.

Allergies There have been reports of rash and pruritus.

Warnings Suicidal behavior and ideation have been observed as early as one week after starting treatment with lacosamide, and is an adverse reaction to the use of most AEDs. In clinical trials with a medial treatment duration of 12 weeks, the incidence of suicidal ideation was 0.43% among 27,863 patients as opposed to 0.24% among 16,029 placebo-treated patients. Suicidal behavior was observed in 1 of every 530 patients treated.

In pregnancy In a study conducted to assess the teratogenic potential of AEDs in the zebrafish embryo, the teratogenicity index of lacosamide was found to be higher than that of lamotrigine, levetiracetam, and ethosuximide. Lacosamide administration resulted in different malformations in the neonatal zebrafish depending on dosage.

Overdose There is no known antidote in the event of an overdose.

Pharmacology

Pharmacodynamics Lacosamide is a functionalized amino acid that produces activity in the maximal electroshock seizure (MES) test, that, like some other antiepileptic drugs (AEDs), are believed to act through voltage-gated sodium channels. Lacosamide enhances the slow inactivation of voltage-gated sodium channels without affecting the fast inactivation of voltage-gated sodium channels. This inactivation prevents the channel from opening, helping end the action potential. Many antiepileptic drugs, like carbamazepine or lamotrigine, slow the recovery from inactivation and hence reduce the ability of neurons to fire action potentials. Inactivation only occurs in neurons firing action potentials; this means that drugs that modulate fast inactivation selectively reduce the firing in active cells. Slow inactivation is similar but does not produce complete blockade of voltage gated sodium channels, with both activation and inactivation occurring over hundreds of milliseconds or more. Lacosamide makes this inactivation happen at less depolarized membrane potentials. This means that lacosamide only affects neurons which are depolarized or active for long periods of time, typical of neurons at the focus of epilepsy. Lacosamide administration results in the inhibition of repetitive neuronal firing, the stabilization of hyperexcitable neuronal membranes, and the reduction of long-term channel availability, but does not affect physiological function. Lacosamide has a dual mechanism of action. It also modulates collapsin response mediator protein 2 (CRMP-2), preventing the formation of abnormal neuronal connections in the brain. Lacosamide does not affect AMPA, kainate, NMDA, GABAA, GABAB or a variety of dopaminergic, serotonergic, adrenergic, muscarinic or cannabinoid receptors and does not block potassium or calcium currents. Lacosamide does not modulate the reuptake of neurotransmitters including norepinephrine, dopamine, and serotonin. In addition, it does not inhibit GABA transaminase.

… excerpt ends here. Continue reading the full article.

Illustrations

Worked examples

Example 1 — a first encounter with Lacosamide

Start with the simplest possible case. Write down what Lacosamide claims or describes in one sentence, then invent the smallest concrete situation in which that sentence is true. In chemistry, the smallest case is usually a single object, a single equation or a single measurement. Check that every symbol or term in your sentence has a meaning in that case.

Example 2 — changing one variable

Take the situation from Example 1 and change exactly one quantity: double it, halve it, or set it to zero. Predict what should happen to Lacosamide before you calculate. Comparing your prediction with the result is the fastest way to find out whether you understand the idea or only the words.

Example 3 — an exam-style question

Typical questions about Lacosamide ask you to (a) state it precisely, (b) apply it to given data, and (c) explain a limitation. Practise writing all three answers in under five minutes; the third part is what separates a full-mark answer from an average one.

Applications of Lacosamide

In research: Lacosamide appears in chemistry research whenever the underlying quantities have to be modelled precisely. Papers usually cite it as a starting assumption and then explore where it breaks down.
In technology and industry: Engineering practice reuses Lacosamide in design rules, simulations and safety margins. Knowing the idea lets you read a specification sheet and understand why the numbers look the way they do.
In the classroom: Lacosamide is common in secondary-school and first-year university syllabi. It links to neighbouring topics Acetamides, Anticonvulsants, Belgian inventions, so understanding it makes those chapters shorter.
In everyday life: Look for Lacosamide outside the textbook — in sport, cooking, traffic, electronics or the sky above you. An example you found yourself is remembered far longer than one you were given.

How to study Lacosamide in 20 minutes

Read the reference excerpt below once, without taking notes.
Close the page and write down what Lacosamide means in your own words.
Compare your version with the excerpt and mark what you missed.
Work through the three examples above with pen and paper.
Explain Lacosamide out loud to somebody else — or to Teacher Smith in the lgStudy chat.

Frequently asked questions

What is Lacosamide in simple terms?

Lacosamide, sold under the brand name Vimpat among others, is a medication used for the treatment of focal-onset seizures and primary generalized tonic–clonic seizures. It is used by mouth or intravenously.

Why does Lacosamide matter?

Because it connects several chemistry ideas at once: it gives you a definition you can apply, a quantity you can calculate, and a way to check whether a result is plausible.

How should I study Lacosamide?

Read the excerpt, restate it from memory, then work through the examples and applications listed on this page. The five-step study plan above takes about twenty minutes.

What does this page cover?

It gives you a compact reference excerpt plus original lgStudy explanations, examples, applications and study material on Lacosamide.