sem 2 pharm 1

• - dentate gyrus of the hippocampus
• - olfactory bulb

• - centrally acting analgesics
• - mu agonist (work on same receptor as endorphins)
• - work on ascending and descending pain tracts
• -(down) DISinhibit GABAs inhib. actions on Ser and NE
• - (up) block NT release from presyn. via blocking Ca channels and hyperpolarize postsyn. via opening K channels
• - Morphine- full mu agonist, full efficacy

- easily discriminable and well localized

- not localized and can only be described generally

• - irreversible COX inhibitor
• - anti-inflammatory, fever, pain, and thrombotic effects
• -**increased risk of bleeding**

• - reversible COX inhibitors
• - inhibit pain and inflammation

• - COX inhibitor in spinal cord and brain
• - reduces pain and fever
• - NO effect on inflammation

- when MOA of the drugs is different

- prevent inflammatory mediator production by working on hormone receptors

• - block neuronal firing
• - effective against nociceptive and neuropathic pain

• - nociceptive and neuropathic pain
• - Lidocaine- Na channel blocker- slow rapid firing of voltage gated Na ion channels
• -Capsacin- substance P- stimulates C fibers- overstimulation causes temporary nerve ending damage, reducing ability to send pain signals

• - act on delta receptors for distraction of pain
• - Nucleus Raphe Magnus will stimulate the release of enkephalins(via seratonin) from inhibitory neurons in spinomesencephalic tract after pain signal reaches PAG via

• - block Ca influx
• - Ketamine- serious side effects like dysphoria and hallucinations

L-tyrosine--(tyrosine hydroxylase** + BioH4)--> L-DOPA

L-DOPA--(DOPA decarboxylase+B6)--> DA

DA--(Cu+ Vit C)--> NE--(SAM)--> Epi

**= irreversible regulatory step

• -taken back up into nerve by high affinity uptake Na cotransport**
• 1. MOA- oxidative deamination
• 2. COMT- methylation
• **= transporter is rate limiting step

• L-Trp--(Trp hydroxylase+BioH4)--> 5-OH-Trp
• 5-OH-Trp--(decarboxylase+B6)-->5-HT(seratonin)

• - can cause HTN when exposed to foods containing tyamine(cheese and redwine)
• - MAO-A for 5-HT(seratonin)
• - MAO-B for DA

• - tricyclic antidepressant
• - inhibit high-affinity uptake of NE and 5-HT(seratonin)
• - approved for use in neuropathic pain
• - side effect- anticholinergic effects
• - not for patients over 65

- inhibit uptake of 5-HT only

-inhibit uptake of DA,NE and 5-HT

- releases DA and 5HT from nerve terminals

• stimulate GABA-A receptor
• - cause increase in Cl conductance
• - hyperpolarize

• - sensitize GABA-A receptor
• ** no suicide risk**
• - increase Cl conductance
• - hyperpolarize

• - SNRI (seratonin, NE reuptake inhibitor
• - approved for peripheral diabetic neuropathy

• - anticonvulsant
• - blocks Ca influx by binding to alpha 2 delta s/u of Ca ion channel
• - blocks release of glutamate and substance P

- lesions to posterior thalamus may cause chronic pain

• - binds to DAT
• - reduces rate of uptake and increases extracellular DA
• - cocaine works this way

• - triggers phosphorylation of DAT causing reversal of DA and subsequent increase
• - inhibits uptake and increases release of DA

• - 6 or more for 6 months
• -often loses thing, creless mistakes, difficulty sustaining attention, poor listener, forgetful, easily distracted, etc

• - 6 or more for 6 months
• - fidgety, cant remain seated, runs about, etc

-regulates selective attention

- sustained attention

- involved in hyperactive sx

- involved in impulsive sx

• - modulates attention processes through arousal networks in the prefrontal cortex
• - also important in behavioral inhibition

-D2 receptor antagonist

• - ez involved in DA metabolism
• -polymorhic (val/met) substitution at gene level increases activity
• - more activity--> less DA

• -synth in rapha nuclei
• - involved in mood, sleep and psychosis
• - can act as excitatory or inhibitory
• - ionotropic or metabotropic
• - therapy target for migraines, anxiety, depression and OCD

• -Seratonin Reuptake Ihnibitor (Ser/Na cotrans inhib)
• - can be used to heal (temporary tx)

• - ligand and metabotropic receptors
• - receptors in basal ganglia, cortex and hippocampus
• -loss of central muscarinic cholinergic neurons-> AD

• -histamine blocker
• - not for pt over 65-> can cause delirium

• - made in locus coeruleus in pons
• - function- arousal, sleep/wake cycle, pain, inflammation, emotions, learning and memory

• - dampens NE tone
• - used in opiate withdrawl
• - can be used in tx of ADD, ax, depresson

• A- ionotropic receptor, increase Cl conductance
• B- metabotropic receptor, increase K conductance