Drugs for Seizures and other Conditions
Document Details
Uploaded by SublimeTuring
Golden State College
Tags
Summary
This document provides detailed information about various drugs used for treating seizures, anxiety, and other related conditions. It covers different types of drugs, their mechanisms, and potential side effects. This is a comprehensive medical guide for drug therapies.
Full Transcript
Other Sedative- Hypnotics Drugs 1\. Z-drugs ZOLPIDEM, ESZOPICLONE, ZALEPLON \*MOA:binds in BZD =which controls sleep/ wakefulness \*DOC for insomnia \*replaced older benzodiazepines for the treatment of insomnia 2\. Melatonin and Related Drugs \* neuroendocrine hormone synthesized in the pine...
Other Sedative- Hypnotics Drugs 1\. Z-drugs ZOLPIDEM, ESZOPICLONE, ZALEPLON \*MOA:binds in BZD =which controls sleep/ wakefulness \*DOC for insomnia \*replaced older benzodiazepines for the treatment of insomnia 2\. Melatonin and Related Drugs \* neuroendocrine hormone synthesized in the pineal gland A. MELATONIN is released before the onset of sleep and produces drowsiness that facilitates sleep. USES b\. treatment of insomnia in shift-change workers -- Graveyard shift B. RAMELTEON (Rozerem) \*acts selectively at melatonin receptors \* approved to treat sleep -- onset insomnia Advantages - No abuse liability - No rebound insomnia 3\. Chloral Hydrate \* older hypnotic that is largely obsolete today \* active metabolite : TRICHLOROETHANOL \* occasionally used for preanesthetic sedation in PEDIATRIC patients 4\. Antihistamines (1^st^ generation) \*DIPHENHYDRAMINE, HYDROXYZINE and DOXEPIN -- insomnia and mild anxiety 5\. BUSPIRONE -treatment of chronic anxiety and produces an anxiolytic effect without causing marked sedation, amnesia, tolerance, dependence, muscle relaxation. 6\. Propranolol \- Treatment of stage fright or acute situational or performance anxiety ANTIEPILEPTIC DRUGS \*Seizure -- abnormal discharge of neurons in the brain. \* Epilepsy -- recurrent, unprovoked seizure. Types of Seizures 1\. Focal Seizures a\. Simple -- no loss of consciousness \- tingling or twitching b\. Complex -- loss of consciousness \- behavioral changes 2\. Generalized Seizures a\. Tonic -- Clonic \- most dramatic \- tonic -- stiffening \- clonic -- muscle contraction alternating with relaxation. b\. Absence Seizures \- primarily affect children \- loss of consciousness c\. Atonic Fall \- loss of tone d\. Myoclonic Seizure \- muscle jerks e\. Status Epileticus \- seizures that lasts longer than 5 minutes f\. Febrile Seizure g\. Epilepsy or Seizure in Pregnancy \- Levetiracetam \- IM MgSO4 -- for eclampsia DRUGS FOR PARTIAL AND GENERELIZED TONIC-CLONIC SEIZURES 1\. CARBAMAZEPINE \* PRODRUG : OXCARBAZEPINE \* DOC -- Partial Seizure, Tic Douloureux ( trigeminal neuralgia ) S/E \*Blood Dyscracias \*Teratogenic \*Passes in breast milk \*Stimulate ADH release \* Steven -- Johnson Syndrome (SJS) 2\. PHENYTOIN \* PRODRUG : FOSPHENYTOIN \* Hydantoin derivative formaly called DIPHENLHYDANTOIN \* DOC for partial seizures A/E - Interferes folate metabolism - Vitamin D metabolism - Collagen metabolism - SJS 3\. VALPROATE \* DOC for tonic clonic seizures \* BROAD SPECTRUM Antiepileptic drug \* FORMS \- Valproic acid = free acid form \- Valproate sodium = sodium salt of valproic acid \- Divalproex sodium = mixture of valproic acid and valproate sodium S/E - Hepatotoxicity ( less than 2 years old) - SPINA BIFIDA 2^nd^ LINE FOR PARTIAL SEIZURE AND GENERALIZED TONIC- CLONIC SEIZURES 1\. PHENOBARBITAL \* PRODRUG : PRIMIDONE -- phenobarbital and phenylethylmalonamide (PEMA) \- act as GABA A receptor agonist \- DOC for FEBRILE SEIZURE or Status Epilepticus in Children ADJUNCT DRUGS FOR PARTIAL SEIZURES 1\. LAMOTRIGINE \* effective adjunct drugs for treating partial seizures in Adults and children. \* treatment in LENOX GASTRO SYNDROME or LENOX GASTAUT SYNDROME -- characterized by multiple types of seizures in pt with mental retardation and other neurologic abnormalities. S/E - Cerebellar dysfunction , drowsiness and rash - SJS - Aseptic meniningtis (rare) 2\. Topiramate \* sulfamate -- substituted monosaccharide \* TERATOGENIC : Cleft palate in Children 3\. Clobazam \* Adjunct treatment of seizures in children and adults with LGS \*Orphan Drug 4\. FELBAMATE \* treatment of Partial seizures refractory to other drugs \*problem: fatal aplastic anemia and acute hepatic failure 5\. Levetiracetam and Brivaracetam \*bind to synaptic vehicle protein (SV2A), reducing vesicular packaging of GABA and impeding neurotransmission across synapses. 6\. Perampanel -- AMDA blockers 7\. Clorazepate 8\. Gabapentin \*treatment of post-herpetic neuralgia \* PRODRUG: GABAPENTIN ENACARBIL \- restless leg syndrome 9\. Pregabalin \* treatment of neuropathic pain \* 1^st^ treatment of FIBROMYALGIA / POST LEG SYNDROME 10\. EZOGABINE \* AKA RETIGABINE \- sodium and chloride channel opener 11\. Vigabatrin \- Block GABA enzyme 12\. TIAGABINE \- GAT -- 1 inhibitor (GABA reuptake inhibition) DRUGS FOR GENERALIZED ABSENCE, MYOCLONIC or ATONIC SEIZURES 1\. ETHOSUXIMIDE \* inhibits the T-type calcium channels \*little toxicity, causes dizziness, drowsiness, gastric distress and nausea \* DOC for ABSENCE SEIZURE in CHILDREN \*in absence seizure, DO NOT USE A.CARBAMAZEPINE B.PHENYTOIN C.GABAPENTIN DRUGS FOR STATUS EPILEPTICUS - OLD DOC : LORAZEPAM - ALTERNATIVE: DIAZEPAM - NEW DOC : MIDAZOLAM \*if uncontrolled by Benzo or phenytoin, use FOSPHENYTOIN \*if highly resistant cases, use GENERAL ANESTHESIA DRUGS FOR PARKINSON'S DISEASE T- TREMOR R-RIGIDITY A-AKINESIA/BRADYKINESIA P-POSTURAL INSTABILTY S-SHUFFLING GAET INTERACTIONS LEVODOPA + MAOIs = Hypertensive Crisis LEVODOPA + Antipsychotic (typicals) = antagonist LEVODOPA + B6 = higher Dopamine conversion LEVODOPA + PROTEINS = transport process alterations LEVODOPA AKA DIHYDROXYPHENYLALANINE OTHER DRUGS for ANTI-PD 1\. AMANTADINE \*antiviral and anti-PD \*MOA = dopamine releaser A/E \*SEDATION, RESTLESSNESS, VIVID DREAMS, LIVEDO RETICULARS ANESTHETIC AGENTS STEPS /STAGES IN ANESTHESIA 1\. CORTICAL- ANALGESIA 2\. DELIRIUM -- NEURONAL EXCITATION 3\. SURGICAL -- RESPIRATORY AND SKELETAL MUSCLE RELAXATION 4\. MEDULLARY -- RESPIRATION DEPRESSION 2 TYPES OF ANESTHETIC AGENTS 1\. LOCAL ANESTHETICS -- block conduction nerve impulses S/E - CNS STIMULATION -- tremors - Drowsiness, sedation - High dose -- seizure or coma A.1 ESTER TYPE LOCAL ANESTHETICS +-----------------------+-----------------------+-----------------------+ | SHORT ACTING "PE" | INTERMEDIATE ACTING | LONG ACTING | | | "BC" | | +=======================+=======================+=======================+ | A. PROCAINE -- 1^st^ | A. COCAINE -- 1^st^ | A. TETRACAINE --long | | synthetic LA | naturally LA | DOA of all ester | | | | | | \*NOT AVAILABLE | \- VASOCONSTRICTOR | | +-----------------------+-----------------------+-----------------------+ | B. CHLOROPROCAINE | B. BENZOCAINE -- | | | | TOPICAL ANESTHETIC | | +-----------------------+-----------------------+-----------------------+ A.2 AMIDE TYPE LOCAL ANESTHETICS +-----------------------------------+-----------------------------------+ | INTERMEDIATE ACTING | LONG ACTING | +===================================+===================================+ | A. LIDOCAINE -- most widely used | A. BUPIVACAINE -- for labor and | | local anesthetic | delivery | | | | | \- safe for pregnant | \- can cause cardiotoxic (most) | | | | | \- soln, ointment, spray, gel, | | | patch | | +-----------------------------------+-----------------------------------+ | B. PRILOCAINE -- congener of | B. LEVOBUPIVACAINE | | lidocaine | | | | \- use for epidural anesthesia | | \- converted to methemoglobin | for labor and delivery | | | | | | \- less cardiotoxic | +-----------------------------------+-----------------------------------+ | EMLA -- LIDOCAINE + PRILOCAINE | C. ROPIVACAINE | | | | | = CIRCUMCISION | \- less potent | | | | | Toxic = methemoglobimia | \- adv: cause fewer cases of | | | cardiac toxicity | | Tx: methylene blue | | +-----------------------------------+-----------------------------------+ | | D. DIBUCAINE -- limited for pain | | | and itchiness | | | | | | E. ETIDOCAINE | +-----------------------------------+-----------------------------------+ B. GENERAL ANESTHETICS \* loss of consciousness a\. MINIMUM ALVEOLAR CONCENTRATION (MAC) \*most potent -- methoxyflurane( 0.16%) \*least potent -- nitrous oxide (100%) b\. BLOOD -- GAS PARTITION COEFFICIENT (BGPC) \*highest BG ratio : METHOXYFLURANE , \*lowest BG ratio : DESFLURANE (0.42%) Example drugs 1\. NONHALOGENATED DRUGS a\. NITROUS OXIDE (laughing gas) \*the only nonhalogenated anesthetic gas used today \*produces greater analgesia than do the other inhalational anesthetics \* NO cardiovascular or respiratory depression \* use in minor surgery A/E \*megaloblastic anemia \* produces mild euphoria 2\. HALOGENATED ANESTHETICS \*halogenated anesthetics replaced older, volatile liquid anesthetics ADVANTAGES \*more rapid rate of induction and recovery \* lower incidence of postoperative nausea and vomiting \*not flammable DISADVANTAGES - Dose dependant respiratory and cardiovascular depression - Cause uterine relaxation - Relatively little analgesia or skeletal muscle relaxation. Examples 1\. HALOTHANE \- the most potent inhalational agent NOW \- disadvan: slow onset and recovery Sensitizes the heart to catecholamines more than other anesthetics HEPATOTOXICITY -- Malignant hyperthermia ( treatment: Dantrolene) 2\. ENFLURANE AND ISOFLURANE \- more rapid induction and recovery than halothane \- less metabolic degradation and produce little cardiac arrhythmia DISADVA: \*cause more respiratory depression APPLICATION - ENFLURANE -- ASTHMA -- least hepatotoxic - ISOFLURANE -- NEUROSURGERY 3\. DESFLURANE AND SEVOFLURANE \*have more rapid rate of induction and recovery than other halogenated anesthetics DESFLURANE- irritating to the respiratory tract SEVOFLURANE -- close to an ideal anesthetic -- preferred for children \*rapid and smooth induction and recovery \* causes little cardiovascular or other organ system toxicity 3\. PARENTERAL ANESTHETICS 1\. BARBITURATES -- thiopental, methohexital 2\. BENZODIAZEPINES --midazolam 3\. OPIOIDS (FENTANYL) FENTANYL + DROPERIDOL = neuroleptanesthesia, twilight sleep FENTANYL + Nitrous OXIDE + DROPERIDOL = neuroleptanalgesia 4\. PROPOFOL \*induction anesthesia, presurgery \* PRODRUG : FOSPROPOFOL \* milk of AMNESIA 5\. ETOMIDATE \*rapid induction to induce anesthesia or for conscious sedation \* no cardiovascular 6\. KETAMINE \*blocks NMDA DISADVAN: unpleasant effects during recovery, including delirium, hallucinations and irrational behavior \*most often used in pediatric patients.