4.5 Miscellaneous drugs
Summary
TLDRThis educational module delves into various anti-epileptic drugs, focusing on their mechanisms of action and classifications. It covers sodium channel blockers like zonisamide, phenobarbital, and lacosamide, each with unique side effects. Potassium channel openers, NMDA and AMPA antagonists, and synaptic vascular protein inhibitors are also discussed, highlighting their specific uses and potential adverse effects. Notably, lamotrigine carries a black box warning due to suicidal tendencies, while levetiracetam is favored for its efficacy and safety in pregnant women. The module concludes with a look ahead to future discussions on epilepsy first aid and management.
Takeaways
- 💊 The module covers miscellaneous anti-epileptic drugs, which are classified based on their mechanisms of action.
- 🔬 Sodium channel blockers are a subclass of drugs, including newer drugs like zonisamide, which has multiple mechanisms including carbonic anhydrase inhibition.
- 🌟 Xenosamide is used for refractory partial seizures and can cause dose-related adverse effects like dizziness and headache.
- 🧬 Aurophinamide is a sodium channel blocker used in epilepsy syndromes, with no drug interactions due to lack of metabolism by microorganismal enzymes.
- 💧 Lacosamide has a dual mechanism of action, inhibiting sodium channels and collapsing receptor-mediated protein, used for partial seizures with dose-related side effects.
- 🔋 Potassium channel openers, like retigabine, prolong after hyperpolarization to reduce neuronal excitability, used for resistant partial seizures with unique side effects.
- 💥 NMDA antagonists, such as felbamate, block NMDA receptors and voltage-gated calcium channels, used for generalized seizures but can cause serious side effects like marrow suppression.
- 🚫 AMPA antagonists, like perampanel, are used for partial seizures and have side effects like weight gain and dizziness.
- 🧠 Levetiracetam modulates synaptic vesicle protein to balance excitatory and inhibitory neurotransmitters, used for various seizure types with fewer side effects.
- 🤰 Levetiracetam is a preferred drug in epilepsy during pregnancy due to its efficacy and safety, available in different strengths for dosage adjustment.
Q & A
What are the main groups of anti-epileptic drugs discussed in the module?
-The main groups of anti-epileptic drugs discussed include sodium channel blockers, potassium channel openers, NMDA antagonists, AMPA antagonists, and synaptic vascular protein inhibitors.
What is the primary mechanism of action of the newer sodium channel blockers like solid graphene glucosamine?
-Solid graphene glucosamine acts primarily by blocking voltage-dependent sodium channels, inhibiting certain types of calcium channels, and causing carbonic anhydrase inhibition.
What are the adverse effects associated with solid graphene glucosamine?
-Adverse effects of solid graphene glucosamine include dizziness, headache, irritability, anorexia, metabolic acidosis, nephrolithiasis, and hypohydrosis, mainly due to its carbonic anhydrase property.
How does xenosamide differ from other sodium channel blockers in terms of metabolism?
-Xenosamide is unique because it is not metabolized by any microorganismal enzymes, unlike first-line sodium channel blockers such as phenytoin or carbamazepine, which means there is no drug interaction with xenosamide.
What is the dual mechanism of action of lacosamide?
-Lacosamide has a dual mechanism of action: it inhibits sodium channels and also inhibits collapsing receptor-mediated protein, which is responsible for the regulation of neurotransmitter release.
What are the side effects of gizagobin, a potassium channel opener?
-Gizagobin can cause physical side effects such as visual disturbances, retinal deposits, and blue pigmentation of nails and lips.
How does felbamate differ from other drugs in its class in terms of mechanism of action?
-Felbamate acts as an NMDA antagonist and also blocks voltage-gated calcium channels, which is different from other drugs in its class that may target different receptors or mechanisms.
What are the potential serious side effects of felbamate?
-Felbamate has potential serious side effects including bone marrow suppression and hepatotoxicity.
What is the mechanism of action of perampanel, an AMPA antagonist?
-Perampanel blocks AMPA receptors, which is different from NMDA antagonists, and it is used in treating partial seizures.
What is the unique mechanism of action of levetiracetam?
-Levetiracetam modulates the effect through synaptic vascular proteins, balancing the excitatory and inhibitory neurotransmitters by binding to these proteins.
Why is levetiracetam preferred in epilepsy treatment during pregnancy?
-Levetiracetam is preferred in epilepsy treatment during pregnancy due to its improved efficacy and fewer adverse effects compared to other drugs, making it a first-line drug option.
Outlines
💊 Overview of Anti-Epileptic Drugs
This paragraph introduces the final module on anti-epileptic drugs, focusing on miscellaneous drugs. It reviews previously discussed drug groups like sodium channel blockers, calcium channel blockers, and those affecting the gamma-aminobutyric acid (GABA) system. The paragraph emphasizes the classification of drugs based on their mechanisms of action, including newer sodium channel blockers, potassium channel openers, and drugs affecting glutamate receptors. It also touches on synaptic vesicle protein inhibitors. Specific drugs like zonisamide, phenomena, retigabine, and the potential side effects of these drugs are mentioned, highlighting their use as add-on treatments for various seizure types. The paragraph concludes with a note on the black box warning for one of the drugs due to its association with suicidal tendencies.
🧠 Mechanisms of Anti-Epileptic Drugs
The second paragraph delves into the mechanisms of action of various anti-epileptic drugs. It discusses the role of glutamate and its receptors, including AMPA and NMDA, in epilepsy. The paragraph describes felbamate and lamotrigine as NMDA antagonists and AMPA receptor blockers, respectively, and their uses in treating specific seizure types. It also covers the side effects associated with these drugs. The paragraph then introduces levetiracetam, a drug that modulates synaptic vesicle protein to balance excitatory and inhibitory neurotransmitters. It mentions levetiracetam's benefits, including its use in pregnancy and its availability in various strengths. The paragraph concludes by setting the stage for the next module, which will cover first aid measures for epilepsy and the management of status epilepticus.
Mindmap
Keywords
💡Anti-epileptic drugs
💡Sodium channel blockers
💡Potassium channel openers
💡Glutamate
💡NMDA antagonists
💡AMPA antagonists
💡Synaptic vesicle protein inhibitors
💡Refractory partial seizures
💡Status epilepticus
💡First aid measures for epilepsy
Highlights
Introduction to the last module on anti-epileptic drugs focusing on miscellaneous drugs.
Discussion on sodium channel blockers as newer drugs in epilepsy treatment.
Mention of solid graphene glucosamine as a sodium channel blocker with multiple mechanisms of action.
Xenosamide's use for refractory partial seizures and its dose-related adverse effects.
Aurophinamide's role in epilepsy syndromes and lack of drug interactions due to its metabolism.
Lacosamite's dual mechanism of action and its use in partial seizures.
Glucosamine's black box warning due to potential suicidal tendencies.
Importance of potassium channel openers in prolonging after hyperpolarization to reduce excitability.
Gizagobin's use in treating resistant partial seizures and its side effects.
Felbamate's action as an NMDA antagonist and its use in generalized seizures.
Perampanel's mechanism of blocking AMPA receptors and its side effects.
Levetiracetam's unique mechanism of modulating synaptic vesicle protein and its broad use in epilepsy.
Levetiracetam's preference in epilepsy treatment during pregnancy and its availability in various strengths.
Conclusion of the module on anti-epileptic drugs and a preview of the next module on epilepsy first aid measures.
Transcripts
welcome students to the last module of
the anti-epileptic drugs where we will
be discussing the miscellaneous drugs we
have already discussed the different
groups of drugs like sodium channel
blockers the calcium channel blockers
and rocks affecting karma system in this
module we will be discussing
miscellaneous drugs
when it comes to the messaging
structures mainly we are going to
enumerate the drugs and we want to
discuss the few salient features of this
drugs in this module
and they are classified again into the
different
subclasses depending on mechanism of
action
and sodium channel blockers we have
already discussed the important uh the
previous drugs but uh here these are the
few newer drugs which are acting by
sodium channel blockers that is zones or
phenomena
potassium channel openers like izuka
bean or reticular bean
and the drugs which affects or reduces
the glutamine effect that is nmda
antagonists like falbermate ampa
antagonist like
and
and the last group of drugs that
synaptic vascular protein inhibitors
like levator stem or brevis
whatever is it have
so now coming to each class of drugs
again the sodium channel blockers yes
the newer drugs is solid
graphene glucosamine and i already told
each anti-epileptic drugs yes mainly it
has primarily it has one mechanism
fraction but it acts by a multiple
mechanism here the drug is mainly axed
by
these dependent sodium channels along
with that it inhibits the type of
calcium channels and it also causes
carbonic anhydrase inhibition this is an
important uh
action because it leads to a lot of
other side effects
so it causes ah it's mainly used and all
these drugs are mainly used as a
add-on drugs for the
different kinds of seizures whereas
xenosamide is mainly used for
refractory partial seizures
adverse effects yes it has a dose
related adverse effect of dizziness
headache irritability anorexia but
mainly because of its the carbonic
anhydrase property it causes metabolic
acidosis nephrolithiasis or hypo
hydrosis
so the next drug is aurophinamide it is
also a sodium channel blocker
it is mainly used in epilepsy syndrome
see when we said uh the different types
of seizures the seizures can be
manifested even in form of a syndromes
where it will be associated with the
multiple other features and graphenamide
is a one such drug which mainly acts by
inhibit you know which is mainly acts in
the one type of uh seizure syndrome that
is called as linux just down syndrome
it is not metabolized by any
microorganismal enzymes like
the first line sodium channel blockers
like phenotoid or you know
the carbon muscle
so there is no drug interaction with
this drugs
the third drop in sodium channel blocker
is lacosamat lakosamite is a peculiar
drug which has two mechanism of action
it acts by inhibiting the sodium channel
yes plus it also inhibits collapsing
receptor mediated protein which is
responsible for the regulation of the
neurotransmitter release
it is also used in partial seizures and
it
also has few of the
dose related adverse effects like
dizziness headache nausea over time
so all these
three sodium channel blockers yes they
have been being used
you know nowadays as i don't talk to
other
treatments
but one point with respect to
glucosamine is it has a black box
warning because it can produce a
suicidal tendency
so we discussed sodium channel blocker
and when we were discussing the initial
mechanism of action we said always the
seizure is due to the imbalance between
the excitatory and inhibitory
neurotransmitter
and it also depends on the
depolarization and after
hyperpolarization activity of the neuron
and we all are about for after
hyperpolarization activity of a neuron
potassium channel opening is a very
important
action so gizagobin is a one drug which
is mainly
acts by the potassium channel opener
so prolongs after hyperpolarization
thereby reducing the excitability it is
also used to treat in a partial seizures
in a resistant cases
but remember the point with respect to
the peculiar side effects of physical
being which can be uh you know your
entrance questions it leads to beauty
prolongation retinal deposits blue
pigmentation of nail and lips
so two classes of drugs we have
completed here now coming to the next
class of drugs that is a drug which
reduces the glutamine effect we all know
glutamate is an important excitatory
neurotransmitter and it mainly acts by
different types of receptor like ampa
receptor nmda receptor and
kinetic receptor or
receptor two important receptor in the
action of glutamate is amphi receptor
and nmda receptor
now coming to the felba mate salvamate
is a drug which mainly acts as a nmda
antagonist it also blocks voltage
voltage-gated calcium channel along with
blocking of nmda receptor
where do we use this drug we use it to
immediately generalize dominican
scissors or a partial seizure but
it has particular side effects again or
marrow suppression or hepatotoxicity
the next step is paraphernal or lampanil
which is
used in partial seizures
again and but the mechanism of action is
opposite to that of feldman or quite
different from that because it blocks
ampa receptor not a nmda receptor but it
also has a side effects of weight gain
dizziness and soreness
uh
i think coming to the last drug in
anti-epileptic group liver is attack it
is a one peculiar drug which has a you
know specific mechanism of action of
modulating the effect through your
synaptic vascular proteins you see here
beta excitatory synapses beta inhibitory
synapses levitosetting tries to modulate
this synaptic muscular protein and
modulates the or modifies the release of
this glutamate or a gaba binding to the
release by binding to this proteins
thereby it balances the excitatory and
inhibitory neurotransmitters
so it also has adverse effects of
dizziness and solutions again used uh
generalized from the cloning species
complex
participants see and levitation is
nowadays being uh one of the important
drug or one of the what we say
uh the first line uh drug because of its
own advantage and improve efficacy and
it is also one of the drugs preferred in
epilepsy in the pregnancy it is
available in uh the different
strengths as tablets and those can be
adjusted depending on the body weight
basis also so there we complete the
module on anti-epileptic drugs so once
we've discussed all these anti-epileptic
drugs in the next module we shall
discuss
uh what is the first aid measures for
epilepsy or how do we generally measure
different types of epilepsy sutures and
how do we
manage our
important emergency condition that is a
status
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