Cumulative Pharm Exam

Direct Acting - ACH Agonists

Bethanechol

Pilocarpine

Nicotine

Indirect acting AChE Inhibitors

Butyrylcholinesterase

keeps ACH in the synapse

Used in MG and Alzheimer’s

What happens at high doses of cholinomimetics?

SLUDS

Salivation, Lacrimation, Urination, Defecation, Sweating

What do cholinomimetics do?

Inc cholinergic signaling

no CNS impacts

Bethanechol

Used for B/B incontinence

CI - Asthma

AE - SLUDs

Pilocarpine

Muscarenic agonist

Miosis (constriction) and decreases intraocular pressure (glaucoma Tx)

eye drops

Nicotine

Enhances memory, learning, alertness, suppresses appetite

AE: GI issues, irritability, Inc BP and HR

Reversible AChE Inhibitors

Neostigmine & Pyridostigmine (and carbaryl)

Similar actions to Bethanechol ( B/B incontinence)

Irreversible AChE Inhibitors

Organophosphate & thiophsophates

Covalently bonds to body leading to SLUDS, Fasciculations and seizures

Antidote for thiophosphates

2-PAM

Must be given quickly to remove covalent modification

Anticholinergics

Atropine - Antidote for AChE inhibitors

Scopolamine - Motion Sx

Ipratropium & Tiotropium (COPD)

Oxybutynin & Tolterodine - OAB

Botox

Disrupts SNARE complex, longer acting

TX for paralysis, dystonias, hyperhydrosis, overactive bladder

Where r H1 receptors located and what is their function?

Located in most smooth mm, vascular endothelium, exocrine gland, and CNS

mediates inflammatory response with bronchochonstriction, dilation

Where are H2 receptors located

Stomach, heart, immune system and acid

Anaphylaxis

Major histamine release - flushing, hives, bronchospasm, hypotension

TX- epinephrine via functional antagonism

1st gen Antihistamines

Dipenhydramine

Dimenhydrinate

Hydroxyzine

Promethazine - nausea and motion sickness

Less specific & more systemic effects, shorter T1/2, crosses BBB

competitive antagonists

Anticholinergic Toxidrome

Excess antihistamine intake

Pt is excessively sleepy and confused

AE of 1st gen antihistamine

Fatigue, dry mouth, mictuition

CNS and Antimuscarenic properties

2nd gen antihistamines

Fexofenadine

Loratadine

Ceterizine

specific to H1, longer T1/2, slower onset

COX-2 Function

Inflammatory response gene

Wider substrate to COX 1, has more room for things to bing

How do NSAIDs work

Inhibit COX

NSAIDS

Aspirin

Ibuprofen & Naproxen (non-selective and OTC)

Celecoxib & Meloxican (cox-2 selective & prescription only)

What does aspirin do?

Irreversibly inhibits COX-1 & 2

Decreases platelet aggregation

Decreases Fever (crosses BBB)

AE of Asprin

GI!! Stomach bleeding, Reye’s syndrome (peds tinnitus, HA, vomit, coma, hallucinations & hyperthemia)

Cox Inhibitors

Ibuprofen & Naproxen (OTC & non selective)

Celecoxib & Meloxicam (cox2 specific & prescription)

Celecoxib

used for arthritis and P!

Less GI impact, NO CV impact

CI - Sulfonamide allergy

Acetaminophen MOA

Weak peripheral COX inhibitor

NOT AN NSAID

What are the dangers of acetaminophen?

Hepatic necrosis

No GI impact, anti-platelet, or reyes syndrome

Acetaminophen/Tyelonol

Analgesia, dec fever, headaches

NSAID Ci

Pregnancy

Liver/renal disease

Bleeding disorders

<18 YO (asprin only)

NSAID caution

>65 yo

GI issues

HTN

Liver/alc abuse

Diuretic use

Function of Glucocorticoids (GCs) in pharm

Powerful anti inflammatory & immunosuppressor

Stimulate surfactant production in fetus

Decrease bone remodeling

increase fuel in last a via increase of gluconeogenisis and fat absorption

GCs Absolute CI

Systemic infections

Severe diabetes

emotionally unstable

Severe CV/renal issues

Peptic ulcers

GCs relative CI

Arrested Tb

Mild diabetes

osteoporosis

convulsive disorders

GCs

Cortisol

Prednisone

Methylprednisolone

Triamcinolone

Dexamethasone

Therapeutic uses of GCs

Replacement therapy (addison’s disease)

Chemotherapy

Stim lung maturation

Allergy

Asthma

Transplant rejection

Autoimmune disorders (RA, ulcerative colitis, MS)

Inflammatory disorders (tendinitis, bursitis, plantar fasciitis)

What are GCs Ae on skin

Skin thinning/ easier bruising

Delayed wound healing

important with topical steroids

AE of GCs

Adrenal insufficiency

Inc appetite

Weakened connective tissue

Peptic ulcers

MM wasting and weakness

OP

Ophthalmic - glaucoma/cataracts

Inhibiting growth

Inc infection susceptibility - will not show typical signs