Non epinephrine

Dopamine

Acetylcholine

Glutamate

Aspartate

GABA

Glycine

Pharmacology of the new drug is determined in the patients with the intended clinical condition

Principal aim is to define relationship beween dose and pharmacological and/or therapeutic response in humans

Main clinical trial

Drug is compared to placebo, or if this would be unethical (effective treatment for the disease in question already exists), an established drug in use for this disease

Postmarketing serveillance

Ongoing monitoring of drug safety under actual conditions of use in large numbers of patients (pharmacovigilance)

A movement disorder that has the following four cardinal characteristics

restin tremours

muscle rigidity

bradykinesia

abnormal gait and posture

Levodopa

Carbidopa

Amantadine

Selegiline

What are the two major categories of sedative-hypnotic drugs?

What is the pathophysiology of both?

Barbiturates

Benzodiazepines

Both enhance the ability of NT, GABA to activate a type of receptors known as GABA-A receptors

Benzodiazepines are useful in chronic therapy of epilepsy.

True or False?

What drug reverses the effect of benzodiazepines?

How is it taken and what is its pathophysiology?

What are its side effects? (4)

Flumazenil

Taken by IV route

It is a GABA receptor antagonist

Nausea, vomiting, agitation and dizziness

Sleep disorder (long acting drug)

List few points about it.

Flurazepam

Duration: Increased

Rebound insomnia: less

Half life: 85 hours, long

SE: daytime sedation

Sleep disorder (intermediate acting drug)

What does it do?

Temazepam

Wakening frequency decreased

Sleep disorder (short acting drug)

List some points.

Triazolam

Sleep induction is good

Rebound insomnia is high

What does zolpidem do?

What kind of drug is it?

What is its half life?

What are its side effects? (3)

Other points about it.

It acts on BZ receptors

It is a hypnotic drug.

Half life: 3 hours, short

SE: Nightmares, GI upset, daytime drowsiness

Onset of action is fast.

No anti convulsant, no muscle relaxation

Amphetamine

Caffeine

Cocaine

LSD

Nicotine

Methylphenidate

Methylxanthine

Cause excitement/ euphoria

Increase motor activity

Important as drugs of abuse

What is the mechanism of methylxanthine?

What does it do?

Increase cAMP (translocation of extracellular calcium)

Causing decreased fatigue and increased mental alertness (relaxation)

Increase CNS/ peripheral action of catecholamines

Blocks reuptake

Intense euphoria

(dopaminergic effect)

What is the mechanism of methlphenidate?

What is its use?

Mechanism: same are amphetamine

Use: narcolepsy/ADD (good in addictive environment)

What is the mechanism of TCA?

What does TCA's interaction with Mao inhibitors do?

block NT reuptake

Hypertensive crisis and tachycardia

OCD

Panic disorders

Agoraphobia

Tranylcypromine

Phenelzine

Clorgyline

Isocarboxazid

depression

parkinsons

narcolepsy

phobia

anxiety

What is the use of SSRI?

Give an example.

Use: any form of depression

Ex: Fluoxetine

Mania

depression

thyroid function

Hemodialysis (preferred)

Peritoneal dialysis + IV fluids

Relieve pain

Anti-diarrheal (because decreases GI motility)

Anti-tussive (because decreases coughing)

What are the four types of analgesics?

What do each do?

Mu --> high abuse receptor; supra-spinal

Ka --> spinal analgesia; pupil constriction

De --> Euphoria, sedation, pupil constriction

Si --> Opposite from above, dysphoris, hallucinations, CVS stimulation, pupil dilation

Morphine

Fentanyl

Heroin

Morphine

Mechanism?

Use?

SE?

ME: Main Mu agonist

Use: Analgesia; pain relief without loss of consiousness

SE: Common COD in acute opioid overdose

Fentanyl

Mech?

Rapid action

short duration on Mu

100x more powerful

Heroin?

Use?

Potency?

No therapeutic use

2-3x more potent than morphine

Codeine

Use?

Antitussive

New cough meds dont have it due to addictive SE

Naloxone

Naltrexone

Naloxone

Mech?

Route?

reverse effects of opioids (coma/resp depression)

IV route

Naltrexone

Mech?

Route?

Same as naloxone but longer duration of action

Oral route

Anesthesia

4 stages of Anesthesia?

Induction

Maintenance

Recovery

Depth

What are some drugs used in concomitantly with preanesthetic medication?

Give examples where aplicable.

Sedative hyponotics

Antianxiety

Opioids (morphine, fentanyl, merperidine)

Antiemetics (ondansteron)

H2-Antagonists

Gastrokinetic agents

Anticholinergics (atropine)

Inhalation agents (halothane, enflurane-older drugs included chloroform/ether)

Procaine

Cocaine

Tetracaine

Anesthetic

Mech?

Use?

What is the order of nerve block?

SE?

Block NA-channel by binding to specific receptor on INNER portion of channel

Use: In infected patients more of anestheis required (cannot penetrate membrane effectively otherwise); short minor procedure

Loss of pain --> temp/touch/pressure

Severe CVS toxicity (which requires Bupivacaine treatment) and HT/Arrythmia (requires cocaine treatment)

IgG

List 5 distinct points about IgG

Most versatile

Most abundant

Only class of Ig that crosses the placenta

Fixes complement

Binding to cells like macrophages, monocytes, PMNs and some lymphocytes (Fc receptors)

IgA

What does it exist as?

What lining does IgA attach to?

How is it transported in the body?

List some other points about IgA (5 points)

Exists as a dimer

Lining of digestive, respiratory and gastrointestinal tract

Transported through epithelial cells

- 2nd more common serum Ig

- Major class of Ig in secretion, found in breast milk

- Local (mucosal) immunity

- Attaches to microbes before they invade the tissues

- Activates complement

IgM

List 6 points for IgM

Third most common

First Ig to be made by the fetus

First Ig to be made by a virgin B cell

Good complement fixing Ig

Good agglutinating Ig

Beinds to some cells via Fc receptors

IgD

Where is it primarily found?

What does it function as?

What does it help in?

What is it active in?

Found on B cell surfaces

Functions as a receptor for antigen

It may help in immune responses

It may be active in allergic responses

IgE

Where is it primarily found in?

List 3 points about IgE.

Found in tissues and bodily fluids

- Least common serum Ig

- Allergic reactions

- Parasitic helminth diseases

Diazepam

Clonazepam

Clorazepate

How is diazepam taken?

What is it used for?

Slow IV

Status epilepticus

Phenobarbital

Primidone

Febrile convulsions

Simple epilepsy

Grandmal epilepsy

What are the two anti epileptic drugs?

What are they both used for?

Phenytoin: Drug of choice for initial therapy in adults

Carbamazepine: Drug of choice in trigeminal neuralgia

PNS

Brain

Ganglia of SNS

Skeletal muscle

Muscarinic (principally ANS)

Nicotinic (principally skeletal muscle)

Beta 1

Beta 2

Alpha 1

Alpha 2

- Arterial and arteriolar constriction (cutaneous, visceral, skeletal and pulmonary)

- venous constriction

- uterine contraction

- pupillary dilation (mydriasis)

- contraction of radial smooth muscle of iris

- contraction of ureter

- contraction of spleen

- contraction of pilomotor muscles

Inhibition of NE release

Inhibition of ganglionic transmission

Vasoconstriction (quantitatively less important that alpha 1)

Myocardium

SA node

Ventricular conduction system

Adipose tissue

Cardiac stimulation (chronotropic, inotropic, dromotropic)

Stimulation of lipolysis

Stimulation of renin secretion

Vascular smooth muscle of the skin

Smooth mucles of muscles

Smooth mucles of mesentery

Smooth muscles of bronchial tree

- Arteriolar dilation (skeletal muscle, coronary visceral beds)

- Bronchodilation

- Intestinal relaxation

- Uterine relaxation

- Bladder body relaxation

- Decrease of insulin release

- Skeletal muscle tremor

- Stimulation of glycogenolysis

Chief therapeutic uses of

Alpa 1

Alpha 2

Beta 1

Beta 2

Alpha 1

Vascular smooth muscle contraction

Alpha 2

Inhibition of transmitter release

Beta 1

Cardiac stimulation

Beta 2

Vascular smooth muscle relaxation

Bronchiolar smooth muscle relaxation

What is pilocarpine used for?

How does it work?

Used in management of glaucoma and has become the standard initial drugs for treating the closed-angle form glaucoma, effective even in open angle type

Works by opening the trabecular mesh work around schlemm canal

Atropine (mydriatic)

Pilocarpine (miotic)

Pralidoxime (PAM)

(Pyridine - 2 aldoxime chloride)

In opthalmology - mydriactic/ cycloplegic

Spastic disorders of GI and lower UT

To treat organophosphate poisoning

To suppress respiratory secretions prior to surgery

What is homatropine used for?

Is it longer or shorter action that atropine?

Drug of choice when doing investigation of the eye, since it dilates the pupil for a short time only

Shorter

Pirenzepine

- Selective M1 antagonist

- Not as good as H2 antagonists (e.g. cimetidine) or proton pump inhibitors (e.g. omeprazole)

Induces histamine release

Lowers BP

malignant hyperthermia

hyperkalemia

increased intraocular pressure

Acute asthma

anaphylactic shock

open angle glaucoma

increase the duration of local anesthesia

Reduce congestion

Reduce swelling of nasal mucosa