Ketoprofen

It acts by inhibiting the body's production of prostaglandin.

Oxyphenbutazone: one of the metabolites of  phenylbutazone. Apazone.  Similar to  phenylbutazone, but less likely to cause  agranulocytosis

Characteristics of Opioid Receptors

mu₁

Agonists : morphine phenylpiperidines

Actions:  analgesia bradycardia sedation

mu₂

Agonists : morphine phenylpiperidines

Actions:  respiratory depression euphoria physical dependence  

delta

Actions:  analgesia-weak,  respiratory depression

kappa

Agonists: ketocyclazocine dynorphin nalbuphine butorphanol

Actions:  analgesia-weak respiratory depression sedation

Sigma

Agonists: pentazocine

Action: dysphoria -delerium hallucinations tachycardia hypertension

epsilon:

Agonists: endorphin

Actions: stress response acupuncture

α-glucosidase inhibitors
 
acarbose
miglitol

Mechanism

inhibit α-glucosidases in intestinal brush border
delayed sugar hydrolysis
delayed glucose absorption
↓ postprandial hyperglycemia
↓ insulin demand

Clinical use

type II DM
as monotherapy or in combination with other agents

Amoxicillin

a moderate-spectrum

β-lactam antibiotic used to treat bacterial infections caused by susceptible

Mode of action Amoxicillin acts by inhibiting the synthesis of bacterial cell walls. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the cell wall of Gram-positive bacteria. microorganisms. It is usually the drug of choice within the class because it is better absorbed, following oral administration, than other beta-lactam antibiotics. Amoxicillin is susceptible to degradation by  β-lactamase-producing bacteria, and so is often given clavulanic acid.

Microbiology Amoxicillin is a moderate-spectrum antibiotic active against a wide range of Gram-positive, and a limited range of Gram-negative organisms

Susceptible Gram-positive organisms : Streptococcus spp., Diplococcus pneumoniae, non β-lactamase-producing Staphylococcus spp., and Streptococcus faecalis.

Susceptible Gram-negative organisms  Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Proteus mirabilis and Salmonella spp.

Resistant organisms Penicillinase producing organisms, particularly penicillinase producing Staphylococcus spp. Penicillinase-producing N. gonorrhoeae and H. influenzae are also resistant

All strains of Pseudomonas spp., Klebsiella spp., Enterobacter spp., indole-positive

Proteus spp., Serratia marcescens, and Citrobacter spp. are resistant.

The incidence of β-lactamase-producing resistant organisms, including E. coli, appears to be increasing.

Amoxicillin and Clavulanic acid Amoxicillin is sometimes combined with clavulanic acid, a β-lactamase inhibitor, to increase the spectrum of action against

Gram-negative organisms, and to overcome bacterial antibiotic resistance mediated through β-lactamase production.

Organic Nitrates 
Relax smooth muscle in blood vessel
Produces vasodilatation
– Decreases venous pressure and venous return to the heart  Which decreases the cardiac work load and oxygen demand. 
– May have little effect on the coronary arteries CAD causes stiffening and lack of 
–    responsiveness in the coronary arteries 
– Dilate arterioles, lowering peripheral vascular resistance  Reducing the cardiac workload

Main effect related to drop in blood pressure by
– Vasodilation- pools blood in veins and capillaries, decreasing the volume of blood that the heart has to pump around (the preload)
– relaxation of the vessels which decreases the resistance the heart has to pump against (the afterload) 

Indications
- Myocardial ischemia 
– Prevention
– Treatment 

Nitroglycerin (Nitro-Bid)
• Used
– To relive acute angina pectoris 
– Prevent exercise induced angina 
– Decrease frequency and severity of acute anginal episodes

Type 
• Oral - rapidly metabolized in the liver only small amount reaches circulation 
• Sublingual – Transmucosal tablets and sprays 
• Transdermal  – Ointment s 
– Adhesive discs applied to the skin
• IV preparations 

Sublingual Nitroglycerine 
•  Absorbed directly into the systemic circulation,  Acts within 1-3 minutes , Lasts 30-60 min 

Topical Nitroglycerine 
• Absorbed directly into systemic circulation,   Absorption at a slower rate. ,  Longer duration of action 
Ointment - effective for 4-8 hours 
Transdermal disc - effective for 18-24 hours 

Isosorbide dinitrate 
• Reduces frequency and severity of acute anginal episodes
• Sublingual or chewable acts in 2 min. effects last 2-3 hours
• Orally, systemic effects in about 30 minutes and last about 4 hours after oral administration
    
Tolerance to Long-Acting Nitrates 
• Long-acting dosage forms of nitrates may develop tolerance
– Result in episodes of chest pain
– Short acting nitrates less effective 

Prevention of Tolerance 
• Use long-acting forms for approximately 12-16 hours daily during active periods and omit them during inactive periods or sleep 
• Oral or topical should be given every 6 hours X 3 doses allowing a rest period of 6 hours

Isosorbide dinitrate (Isordil, Sorbitrate) is used to reduce the frequency and severity of acute anginal episodes.
When given sublingually or in chewable tablets, it acts in about 2 minutes, and its effects last 2 to 3 hours. When higher doses are given orally, more drug escapes metabolism in the liver and produces systemic effects in approximately 30 minutes. Therapeutic effects last about 4 hours after oral administration

Isosorbide mononitrate (Ismo, Imdur) is the metabolite and active component of isosorbide dinitrate. It is well absorbed after oral administration and almost 100% bioavailable. Unlike other oral nitrates, this drug is not subject to first-pass hepatic metabolism. Onset of action occurs within 1 hour, peak effects occur between 1 and 4 hours, and the elimination half-life is approximately 5 hours. It is used only for prophylaxis of angina; it does not act rapidly enough to relieve acute attacks.