DOC for >65 y Parkinson's

Side Effects: Dyskinesias, On-off motor

MOA: inhibits decarboxylation of peripheral levodopa.

In presence of Carbidopa, crosses blood-brain barrier, is carboxylated into dopamine

<65 y Parkinson's

Side Effects: Confusion, ankle swelling

MOA:  dopamine released from remaining intact dopaminergic terminals in substantia nigra

<65 monotherapy Parkinson's; advanced pt adjunct to L-dopa

Side Effects: postural hypotension, hallucination, drowsiness (esp elderly)

MOA:  directly stimulate dopamine receptors

Parkinson's, adjunct to L-dopa

Side Effects:  GI, dyskinesias

MOA:  inhibit plasma COMT(catechol-O methyl tranferase) enzyme--> prolongs T 1/2 of Levodopa.

adjunct to L-dopa

Side Effects: GI, dyskinesias, elevation of liver enzymes (seldome used, must monitor serial LFT's)

MOA:  COMT inhibitor

young, mild Parkinson's:  tremor, drooling

Side Effects:  anticholinergic S/E=dry mouth, cognitive changes

MOA: antimuscarinic (prevents drooling)

Opioids (see 4/10 Medical Letter)

morphine, codeine, hydrocodone, oxycodone, heroin

moderate to severe pain; postoperative med; adjunct for  anaesthesia; some have antussive, antidiarrheal effects

AVOID in case of ill-defined chronic pain.

Side effects: addiction, constipation; overdose: coma, respiratory depression, miosis ("pinpoint pupils"); hypotension, decreased bowel sounds (acute: nausea and vomiting)

MOA:  agonists at mu, delta, and kappa opioid receptors; primarily through Gi/Go proteins to hyperpolarize neurons and inhibit neurotransmitter release.

opiod overdose

side effects: severe withdrawal if physically dependent

MOA: opioid antagonist

synthetic opioid agonist

fentanyl patch:  for systemic pain, slow release

Side Effects:  meperidine--excessive doses can lead to seizures from excessive accumulation of metabolites (esp if renal function impaired)

to reverse respiratory and CNS depression in suspected overdose

MOA:  displaces opioid narcotics from receptor sites

for opioid addiction and alcoholism (binge drinking, bulimia)

MOA:  longer acting bioavailable opioid antagonist

antidiarrheal agent

MOA: opioid-related

lidocaine, procaine, bupivicaine, cocaine (ENT):

need DURATION OF ACTION

local anaesthesia (dental extraction, suturing), spinal anesthesia, nerve blocks

MOA:  block sodium channels, which prevents generation and conduction of nerve impulses

Combo with vasoconstrictors:  epinephrine, phenylephrine, prolongs duration of action

Lidocaine: widely used, infiltration, prolonged by vasoconstrictors

Procaine: action is transient, allergic response likely (PABA)

Bupivicaine: injectable, long duration (binds to plasma proteins)

Cocaine: naturally occuring from Eythroxylon coca--can cause CNS depression and death (respiratory) following use.  Blocks uptake of catecholamines

1) Know which drugs for which type of seizure (ex: phenytoin makes absence seizures worse)

2) Medical Letter: phenytoin no longer DOC for tonic-clonic or partial seizures

3) Treatment of epilepsy should begin with single drug

4) Difficult to control patients should be seen by a neurologist

valproate (depakote)

DOC for generalized TONIC-CLONIC (Grand Mal) seizure

(mood stabilization effect)

DOC for ABSENCE (Petit Mal) seizure

Side Effects:  nausea/vomiting common (depakote enteric coated=better, also take with food, slow titration); weight gain relatively common; serious effects--uncommon--unexplained heptatoxicity esp <2 y (monitor liver function tests)

MOA: may increase GABA in brain.

DOC for generalized TONIC-CLONIC (Grand Mal)

DOC for ATYPICAL ABSENCE, MYOCLONIC, ATONIC

some adults: monotherapy

children >2 and adults: adjunct for partial seizures

Side Effects:  rash (Stevens-Johnsons' Syndrome: severe, diffuse, involvment of mucosal surfaces).  Risk of rash high if hi dose, dose increased too fast, or given w/ valproate.  discontinue at first appearance of rash.

MOA: ?

DOC for TONIC-CLONIC (Grand Mal)

DOC for PARTIAL, including secondary generalized seizures

DOC for ATYPICAL ABSENCE, MYOCLONIC, ATONIC

adults and children >4 y w/ partial seizures

adults and children > 6 y w/ primary generalized seizures--TONIC CLONIC

adults and children > 12 y w/ myoclonic seizures

Side Effects:  somnolence, dizziness, weakness, irritability but not life-threatening. Few drug-drug interactions (not metabolized by CP450)

MOA:  selective binding to synaptic vesicular protein SV2A (may modify synaptic release of glutamate, GABA)

DOC for PARTIAL, including some secondary generalized seizures

Side Effects:  rashes w/ high doses (Stephen Johnson).  Asians at risk for severe skin rashes (test for HLA-B1502 in advance)

CNS (drowsiness, headache, decreased cognitive function)

mild leukopenia, hyponatremia

many drug-drug interactions

MOA:  may reduce polysynaptic responses and block post-tetanic potentiation.  Treat chronic pain of trigeminal neuralgia and diabetic neuropathy.

DOC for PARTIAL, including secondary generalized seizures

may WORSEN some patients with ABSENCE absence

Side Effects:  Rashes, esp w/ hi doses, Asians at risk for severe skin rashes (test for HLA-B1502 in advance).  CNS (drowsiness, headache, decreased cognitive function)

MOA:  reduces polysynaptic responses and blocking post-tetanic potentiation.  Also used to treat chronic pain of trigeminal neuralgia and diabetic neuropathy

DOC for ABSENCE (Petit Mal)

Side Effects:  well tolerated (nausea, vomiting, hiccups)

MOA: ?

second-line drug, previously DOC for generalized tonic-clonic and partial seizures

Side Effects:  complicated pharmacokinetics.  Nystagmus, drowsiness, ataxia, diplopia, rash/hypersensitivity, gingival hyperplasia

MOA:  may block sodium channels (stabilize threshold against hyperexcitability).  Blocks calcium channels.  May enhance GABA.

combination Rx, chronic pain syndromes

Side effects:  few drug-drug interactions

adjunctive theapy for variety of seizures

phophylactic for migraines

treatment for neuropathic pain

Side Effects:  paresthesisas, cognitive impairment; chronic use may cause metabolic acidosis, increasing risk of renal calculi

MOA:  carbonic anhydrase inhibitor

diazepam (see benzodiazepines)

single-dose prefilled syringes

Diastat:  new rectal formulation

repetitive seizures (rapidly absorbed, effective for acute seizures, can be used in combo with other antiepileptics)

may decrease ER visits

Side Effects:  ? make seizures worse

MOA:

Natural Standard A grade for dementia

B grade for cerebral insufficiency

Side Effects:  bleeding as montherapy, in combo

MOA:

 B for improving mental performance

Side Effects:  bleeding as monotherapy and combo, care when combo with cardiac drugs