Mechanisms Flashcards
(42 cards)
Opioids
3 opioid receptors : mu , delta , kappa Natural endogenous opioids are : Enkephalins Dynorohins Endorphins
Endorphins act on u
Closing of voltage gated Ca channels and open K channels allowing efflux of K ions.
Opioids Adverse effects
Nausea Vomiting Anti tussive Respiratory depression Immune Suppression Constipation Flushing (meperidine morphine) Itching Urinary retention Dependence
Buprenorphine
Partial agonist of u rec
Antagonist of k and d rec
Produces partial effect thus less risk of abuse
Naloxone
Opioid antagonist
Morphine antidote
Anesthesia stages
- Induction
- Excitement
- Surgical Anesthesia
- Medullary paralysis
1st group Anesthesia
Etomidate
Propofol
Barbiturates
Unconsciousness more then analgesia
Act on GABA a
Hyperpolarization of resting potential . Open Cl channels, suppress neuronal excitability .
Used in Induction phase.
1st group Anesthesia Adverse effects
Etomidate
Renal suppression
Transient Skeletal muscle movements (myoclonus)
Propofol
Respiratory depression
Hypotension
Barbiturates
Bronchospasm
Respiratory depression
2nd group Anesthesia mech
Ketamine (IV)
Nitrous Oxide
Xenon
Cyclopropane
No effect on GABA
More Analgesia than unconsciousness
Ketamin
Act on N-methyl D aspartate rec NMDA
Inhibits NDMA receptors. Inhibit glutamate excitatory action
Xenon
Cyclopropane
Selectively inhibit NMDA
2 pore domain K channels . Efflux of K ions
2nd group adverse effects
Ketamine: Htn tachy Hypersalivation Hallucinations Delrium
Nitrous oxide , cyclopropane
Dizziness nausea vomit
Xenon: none
3rd group
Halothane Enflurane Isoflurane Sevoflurane Desflurane
Act on all
GABA a, NMDA & 2 pore domain K channels and many other
3rd group side effects
Dose dependant hypotension
Low cardiac output
Arrhythmia hepatotoxicity (halothane)
Renal toxicity ( Sevoflurane)
Dexmedotomidine
Unique Anesthetic
Presynaptic a2 adrenergic rec
Brady
Hypotension
Local anesthetics mechanism
Bind to a site on voltage gated Na Channels prevention of Na Influx .
Local anesthetics adverse effects
Systemic effects: Blurry vision Light headedness Seizure Cardiac arrhythmia
Alzheimer’s drugs mechanisms
Anti cholinesterases
Rivastigmine ( both Acetyl and butyl cholinesterase)
Donapezil
Galantamine
Tacrine
Inhibit cholinesterase enzyme and promotes prolonged action of Ach
NMDA rec antagonist
Memantine
Abnormal B -amyloid accumulation may cause high levels of glutamate by inhibiting it’s uptake and triggering more release from glial cells.
Memantine binds to NMDA receptors and block excitatory action of glutamate by blocking Ca influx
Side effects Alzheimer’s
Anti cholinesterase
SLUD
Brady
Weight loss
Memantine
Insomnia
Diarrhea
Headache
Parkinson’s mechanism
Parkinson’s develops when neurons connecting substantia Niagra to striatum degenerate
Dopaminergic neurons originate in substantia niagra
Low dopamine causes more GABA & more Ach
Increase inhibition in thalamus and reduced excitatory input to motor cortex
Parkinson’s drugs mechanisms
Pre BBB crossing
Tyrosine –th–> L-Dopa –AADC–> DOPAMINE
DOPAMINE released
Broken by MAO-B and COMPT
Levodopa (precursor of Dopamine) (BBB crossing)
Carbidopa (inhibits Dopamine Decarboxylase)
Entacapone (inhibits COMPT)
Parkinson’s drugs mechanisms
Post BBB
Selegeline
Rasagiline
Inhibit MAO-B
Tolcapone: inhibits COMT
Parkinson’s drug mechanism
Anti Muscarinic Agents
Benztropine
Biperidine
Procyclidine
Trihexphenidyl
Parkinson’s drugs
Dopamine mimics
Bromocriptin Ropinorole Pramipexole Rotigotine Apomorphine
Stimulate dopamine receptors to produce similar effects as dopamine
Amantadine Parkinson’s
Facilitates pre synaptic dopamine release
Blocks Glutamate NMDA rec