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Pharmacology

Streptomycin

Streptomycin was the first of a class of drugs called aminoglycosides to be discovered, and was the first antibiotic remedy for tuberculosis. It is derived from the actinobacterium Streptomyces griseus.

Streptomycin cannot be given orally, but must be administered by regular intramuscular injection.

Phenytoin (Dilantin): for tonic-clonic and all partial seizures (not effective against absence seizures)


Mechanism: ↓ reactivation of Na channels (↑ refractory period, blocks high frequency cell firing, ↓ spread of seizure activity from focus)


Side effects: ataxia, vertigo, hirsutism (abnormal hair growth), gingival hyperplasia, osteomalacia (altered vitamin D metabolism and ↓ Ca absorption), blood dyscrasias (rare; megaloblastic anemia, etc)


Drug interactions: induces hepatic microsomal enzymes (can ↓ effectiveness of other drugs); binds tightly to plasma proteins and can displace other drugs

Antiemetics

 Antiemetic drugs are generally more effective in prophylaxis than treatment. Most antiemetic agents relieve nausea and vomiting by acting on the vomiting centre, dopamine receptors, chemoreceptors trigger zone (CTZ), cerebral cortex, vestibular apparatus, or a combination of these.
 
 Drugs used in the treatment of nausea and vomiting belong to several different groups. These include:
 
1. Phenothiazines, such as chlorpromazine, act on CTZ and vomiting centre, block dopamine receptors, are effective in preventing or treating nausea and vomiting induced by drugs, radiation therapy, surgery and most other stimuli (e.g. pregnancy).
They are generally ineffective in motion sickness.
Droperidol had been used most often for sedation in endoscopy and surgery, usually in combination with opioids or benzodiazepines

2. Antihistamines such as promethazine and Dimenhyrinate are especially effective in prevention and treatment of motion.

3. Metoclopramide has both central and peripheral antiemetic effects. Centrally, it antagonizes the action of dopamine. Peripherally metoclopramide stimulates the release of acetylcholine, which in turn, increases the rate of gastric. It has similar indications to those of chlorpromazine.

4. Scopolamine, an anticholinergic drug, is very effective in reliving nausea & vomiting associated with motion sickness.

5. Ondansetron, a serotonin antagonist, is effective in controlling chemical-induced vomiting and nausea such those induced by anticancer drugs. 

6. Benzodiazepines: The antiemetic potency of lorazepam and alprazolam is low. Their beneficial effects may be due to their sedative, anxiolytic, and amnesic properties

Anticonvulsants: include carbamazepine (use when lithium not tolerated; may not be as effective) .

valproic acid (use when lithium not tolerated; rapid onset)

GLP-1 analogs

Exenatide

Mechanism

GLP-1 is an incretin released from the small intestine that aids glucose-dependent insulin secretion
basis for drug mechanism is the observation that more insulin secreted with oral glucose load compared to IV 

Exenatide is a GLP-1 agonist

↑ insulin
↓ glucagon release
the class of dipeptidyl peptidase inhibitors ↓ degradation of endogenous GLP-1
e.g.) sitagliptin, -gliptins 
 

Clinical use
type II DM

 

Toxicity
nausea, vomiting
pancreatitis
hypoglycemia
if given with sulfonylureas

Doxycycline

Commonly prescribed for infections and to treat acne. treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia., as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria.

Hypothalamic - Pituitary Drugs

Somatropin

Growth hormone (GH) mimetic

Mechanism

agonist at GH receptors
increases production of insulin growth factor-1 (IGF-1)

Clinical use

GH deficiency
increase adult height for children with conditions associated with short stature 
Turner syndrome
wasting in HIV infection
short bowel syndrome

Toxicity

scoliosis
edema
gynecomastia
increased CYP450 activity


Octreotide

Somatostatin mimetic

Mechanism

agonist at somatostatin receptors

Clinical use

acromegaly
carcinoid
gastrinoma
glucagonoma
acute esophageal variceal bleed

Toxicity

GI upset
gallstones
bradycardia
Oxytocin

Mechanism

agonist at oxytocin receptor

Clinical use

stimulation of labor
uterine contractions
control of uterine hemorrhage after delivery
stimulate milk letdown

Toxicity

fetal distress 
abruptio placentae 
uterine rupture
Desmopressin
ADH (vasopressin) mimetic

Mechanism

agonist at vasopressin V2 receptors

Clinical use

central (pituitary) diabetes insipidus
hemophilia A (factor VIII deficiency)
increases availability of factor VIII
von Willebrand disease
increases release of von Willebrand factor from endothelial cells

Toxicity

GI upset
headache
hyponatremia
allergic reaction

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