Opiod receptors are this type of receptor, and have these classes:
G-protein coupled receptors (mu, delta, kappa) (μ, δ, κ)
Receptor that binds morphine and endorphins?
Mu (μ) opiod receptor
Receptor that binds enkephalins?
Delta (δ) opiod receptor
Receptor that binds dynorphins?
Kappa (κ) opiod receptor
This drug category/class is used for cough suppression, diarrhea; SE: respiratory depression, miosis, CNS depression (coma), constipation
Opiod drug; MOA: full mu (μ) agonist; SE: histamine release
Opiod drug; MOA: full mu (μ) agonist; other: useful for maintenance, long duration, orally active
Opiod drug; MOA: full mu (μ) agonist; SE: muscarinic antagonist (doesn't cause miosis), don't combine with SSRIs or MAOIs
Opiod drug; MOA: full mu agonist (the other commonly used opiod drug besides morphine)
Opiod drug; MOA: partial mu agonist; given in combination with NSAIDS; antitussive
What are the OTC opiod analgesics?
Dextramethorphan (antitussive), diphenoxylate (antidiarrheal), loperamide (antidiarrheal)
This opiod antagonist has a short half-life; IV; used for acute (emergency) opiod overdose (heroin)
Opiod antagonist; PO; used to reduce ethanol craving (given to alcoholics); also used for long-term opiod addiction
What symptoms does abstinence syndrome (withdrawal from opiods) feature?
Anxiety, GI distress, gooseflesh, muscle spasms, rhinorrhea, sweating
Epilepsy drugs that block Na channels
Phenytoin, carbamazepine, topiramate, lamotrigine, valproic acid
This epilepsy drug blocks Na channels; SE: gingival hyperplasia, hirsutism, hydantoin fetus, megaloblastic anemia (↓ folate absorption)
This epilepsy drug blocks Na channels; SE: Steven-Johnson syndrome
What is a partial seizure?
Simple partial: sensory disturbances; Complex partial: incontinence, post-ictal confusion, déjà vu, lip smacking
What is the DOC for treatment of partial seizures, its MOA and SE?
Carbamazepine (stabilizes the inactivated state of sodium channels and ↑ GABA); SE = blood dyscrasias, teratogenic
What is a tonic-clonic seizure and its DOC?
"Grand-mal" (freeze/jerk); DOC = Valproate (Valproic acid)
What is the MOA and SE of Valproate (Valproic acid)?
↑ GABA; blocks Na channels and T-type Ca++ channels; SE = rare fatal hepatotoxicity, causes fetal NTDs
What is an absense seizure and its DOC?
Blank stare, EEG = 3-Hz spike and wave; DOC = Ethosuximide
What is the MOA and SE of Ethosuximide?
Blocks T-type Ca++ channels; SE: fatigue, GI, headache, Steven-Johnson Syndrome
What is status epilepticus and its treatment?
Continuous seizures >20min. Treatment: Lorazepam → Phenytoin → Phenobarbital → Midazolam/Intubation
What is a febrile seizure and its DOC?
Kids, occurs during rise in temp, not peak temp; DOC = Acetaminophen
What is a temporal seizure and its DOC?
Have hallucinations before seizure; DOC = Carbamazapine
What is a myotonic seizure?
Increased muscle tone, arms fling forward; DOC = Valproic acid (Valproate)
What is a Lennox-Gasteau seizure and its treatment?
Hundreds of seizures every day; DOC = EEG, then lobectomy
This epilepsy drug blocks Na channels and ↑ GABA; SE: kidney stones
These epilepsy drugs block thalamic T-type Ca++ channels
Ethosuximide, Valproic acid
These epilepsy drugs increase GABA
Topiramate, Valproic acid, Benzodiazepines, phenobarbitol, gabapentin
This epilepsy drug ↑ GABA; SE: dependence (first line for acute seizures)
Benzodiazepines (diazepam, lorazepam)
This epilepsy drug ↑ GABA; SE: dependence (first line for pregnant women, children)
This epilepsy drug ↑ GABA; SE: sedation, ataxia
Which acts faster, highly blood soluble anesthetics or low blood soluble anesthetics?
Low solubility in blood = Rapid induction and recovery.
What effect does lipid solubility have on anesthetics?
High lipid solubility = high potency
What effect does minimal alveolar concentration of anesthetics have on their potency?
As MAC increases, potency decreases.
List the inhaled anesthetics and their MOA.
Halothane (→ hepatitis), isoflurane (used in heart sx), NO2 (→ diffusion hypoxia); these block Na channels from inside!
What inhaled anesthetic has hepatotoxicity?
What inhaled anesthetic has nephrotoxicity?
What inhaled anesthetic is a proconvulsant?
This class of drugs increases the duration of Cl- channel opening, thereby facilitating GABA-A action (↓ neuron firing)
This class of drugs increase the frequency of Cl- channel opening, thereby facilitating GABA-A action (↓ neuron firing)
List the benzodiazepines (3ish)
-zepams, zolams, and chlordiazepoxide
This drug is used to treat benzodiazepine overdose and acts as a competitive antagonist at GABA receptor
List the short-acting benzodiazepines (3)
triazolam, oxazepam, midazolam ("TOM thumb")
List the intravenous anesthetics (5ish)
B.B. King on OPIATES PROPOses FOOLishly (Barbiturates, benzodiazepines, Ketamine, opiates, propofol)
This high potency barbiturate is used for induction of anesthesia in short procedures, decreases cerebral blood flow (IV anesthetic)
This benzodiazepine is the most common drug used for endoscopy; may cause severe postoperative respiratory depression (IV anesthetic)
A PCP analog used as a dissociative anasthetic; decreases cerebral blood flow (IV anesthetic)
2 opiates used with other CNS depressants during general anesthesia (IV anesthetics)
Used for rapid induction of anesthesia and short procedures, less postoperative nausea than other drugs (IV anesthetic)
What fibers are affected first by local anesthetics?
Small, myelinated fibers. Pain first, Pressure is last.
What do you co-administer with local anesthetics and why?
Vasoconstrictors [Epi] to enhance local action (except cocaine!)
What are the local anesthetics (5) with a short half-life?
Esters (cocaine, benzocaine, procaine, tetracaine, novacaine)
What are the local anesthetics (5) with a long half-life?
Amides ("two i's" - Lidocaine, Prilocaine, Mepivacaine, Bupivacaine)
Local anesthetics MOA
Block Na channels (preferentially bind activated Na channels)
What local anesthetics causes CNS excitation and severe cardiovascular toxicity?
What are neuromuscular blocking drugs used for?
Muscle paralysis in surgery or mechanical ventilation.
What receptor do NMJ-blocking drugs target?
NMJ-blocking drugs block transmission at the neuromuscular junction, causing paralysis of the affected skeletal muscles, either by acting presynaptically via the inhibition of ACh synthesis/release or by acting postsynaptically at the ACh receptors.
What is the only depolarizing NMJ-blocking drug and what are its two phases?
Succinylcholine. Phase 1 = prolonged depolarization. Phase 2 = Repolarized but bloacked.
Effect of giving cholinesterase inhibitors in each phase of succinylcholine action.
Phase 1: Cholinesterase inhiitors makes it worse. Phase 2: Reversed by cholinesterase inhibitors
What are the nondepolarizing NMJ blockers?
Have cur in the name (end in cararine, curium or curonium)
How do you reverse a nondepolarizing NMJ block?
ACh-E inhibitors (neostigmine, edrophonium)
How do you treat malignant hyperthermia or neuroleptic malignant syndrome? (same drug)
Dantrolene (prevents release of Ca2+ from SR)
What causes malignant hyperthermia?
Using inhaled anesthetics (except NO2) + succinylcholine)
What are the drugs used for Parkinson's treatments?
BALSA (Bromocriptine, Amantadine, Levodopa, Selegiline, Antimuscarinics)
What are the 4 treatment classes for Parkinson's?
Agonize dopamine receptors (bromocriptine), ↑ Dopamine (Amantadine, L-dopa/carbidopa), Prevent dopamine breakdown (MAO-B inh, selegiline), Curb excess cholinergics (benztropine, no effect on bradykinesia)
What is the treatment for essential or familial tremors?
How does the L-dopa/carbidopa treatment work?
L-dopa crosses the blood brain barrier and is converted in CNS to dopamine. Carbidopa inhibits peripheral decarboxylase.
What Parkinson drug causes arrhythmias?
L-dopa (when it's converted to dopamine in periphery)
What drug is co-administered with L-dopa in Parkinson's but may enhance its side effects?
Selegiline (MAO-B inhibitor)
DOC for treatment of migraines, its MOA and SE?
Sumatripan. 5-HT 1D agonist. Causes vasoconstriction. Short half-life. SE: coronary vasospasm
Contraindications for sumatripan?
CAD or prinzmetals (causes coronary vasospasm)