1. Blockade of adenosine receptors

2. Increase in cAMP by inhibition of phosphodiesterase

1. The seizure threshold is lowered

2. It can be useful in ECT for psychiatric paitents (Electroconvulsive therapy)

1. Drowsiness

2. Fatigue

3. Neonatal Apnea

4. Asthma

5. Lumbar puncture headache

1. Low doses: Ganglionic stimulation by depolarization

2. High doses: Ganglionic blockade

1. Benzoic-acid ester

2. Mechanism of action: blocks the reuptake of monoamines (Nepi, serotonin, dopamine)

3. Unique: no other local anesthetic blocks Nepi reuptake. Makes it useful for surgical procedures because it causes vasoconstriction (ENT surgeons use it intranasally b/c it provided anesthesia and decreased bleeding).

Discuss question 10.1. What is the general approach to the treatment of cocaine toxicity?

Question 10.1:A very agitated young male was brought to the emergency toom by the police. Psychiatric exam revealed that he had snorted cocaine several times in the past few days, the last time being 10 hours previously. He was given a drug that was used to counter this patient's apparent cocaine withdrawl is:

* Drug of choice to treat ANXIETY/AGITATION of cocaine withdrawl is a benzodiazepine, LORAZEPAM.

* General approach to treatment of cocaine toxicity: decrease CNS and cardiovascular effects of drugs.

1. BENZO: Agitation, anxiety, seizures (Ativan/Versed)

2. Na + bicarb: rhabdomyolysis dysrrhythmias

3. Lidocaine: treat cocaine induced VF or VT

4. Bretylium: treat PVC

5. NTG: treat HTN and cardiac chest pain

6. Nitroprusside: treat HTN

7. Norepinephrine: treat hypoTN unresponsive to IVF

* Esmolol (brevibloc) contraindicated, but some recommend use with vasodilator ONLY to manage life threatening HTN, tachycardia, aortic dissection.

A 30 year old male presents with chest pain following cocaine administration. EKG is remarkable for multifocal PVC's. What medication would you use to treat this patient?

1. Bertylium to treat PVC's

2. NTG to treat cardiac chest pain

3. Benzodiazepines to treat agitation

Make sure to address:

• Agitation
• HTN
• arrhythmias
• coronary ischemia caused by vasospasm

What is the mechanism of action and toxic side effects of amphetamines?

1. Depend on elevated levels of catecholamine neurotransmitters in the synaptic spaces.

2. Release intracellular stores of catecholamines

3. Causes behavior effects from combo of dopamine and Nepi release

4. Indirectly stimulate Adrenergic receptors via Nepi release

• increased alertness
• decreased fatigue
• decreased appetite
• insomnia
• HIGH DOSES: psychosis and convulsions

What are the therapeutic uses of amphetamines?

Treatment of:

• ADHD
• narcolepsy
• treatment resistant depression
• weight loss management

Summarize the pharmacology of methylphenidate?

RITALIN:

• Block reuptake of dopamine and Nepi into the presynaptic neuron
• Increases the release of dopamine and Nepi into the synaptic space

Describe the pharmacologic treatment of narcolepsy.

1. Amphetamines enhance Nepi and dopamine release

2. Methylphenidate blocks Nepi and dopamine reuptake

Summarize the pharmacology of LSD, cannabis, and phencyclidine (PCP).

LSD: binds to and activates serotonin receptors causing an exaggerated activation of the receptor.

• Causes: rapid mood swings, altered perceptions, delusions

Cannabis: (THC) act on cannabinoid receptors and stimulating the release of dopamine.

PCP: works on NMDA (n-methyl d aspartate) receptor antagonist blocking the activity of the NMDA receptor.