PRAMIPEXAZOLE - ANTIPARKINSONIAN DRUG

                                                                          PRAMIPEXOLE

MECHANISM OF ACTION –

 Pramipexole acts on dopaminergic receptors.

PHARMACOLOGICAL ACTION –

Improvement occurs in parkinsonian patients.

Postural hypotension

Inhibit prolactin release

USES –

1. Treating the signs and symptoms of Parkinson disease.

2. It is also used to treat restless legs syndrome (RLS).

SIDE EFFECTS -

Drowsiness

Hallucinations nausea

Trouble sleeping

Twitching, twisting, or other unusual body movements

Confusion

cough

difficulty with swallowing

double vision or other changes in vision

falling asleep without warning

fearfulness, suspiciousness, or other mental changes

fever

frequent urination

memory loss

muscle or joint pain

muscle weakness

restlessness or need to keep moving

swelling of the body

tightness in the chest

DRUG-DRUG INTERACTION –

Pramipexole + Propoxyphene = may increase side effects such as dizziness, drowsiness, confusion, and difficulty concentration

REFERENCE: Tripathi K.D;'' Essentials of Medical Pharmacology'' ; Seventh Edition ; Page no. 425, 430-31

POSACONAZOLE - ANTIFUNGAL DRUGS

                                                       POSACONAZOLE

MECHANISM OF ACTION- 
It inhibits fungal CYP450 enzyme lanosterol  14- demethylase and thus impairs ergosterol synthesis leading to a cascade of membrane abnormalities in the fungus.

USES-
1. To treat infections by Candida , Aspergillus , or fusarium species.

SIDE EFFECTS-
1. Nausea
2. Abdominal pain
3. Loose motion
4. Headache
5. Dizziness
6. drowsiness

PHARMACOLOGICAL ACTION-
It blocks the synthesis of ergosterol.
It is significantly more potent at inhibiting 14-a demethylase than itraconazole.

DRUG-DRUG INTERACTION-
Posaconazole + H2 blocker = reduce gastric acidity
Posaconazole + phenytoin = decreases metabolism
Posaconazole + PPI = reduce gastric acid Secretion


REFERENCE : Tripathi K.D ;'' Essentials of Medical Pharmacology'' ; Seventh Edition; Page no. - 789, 795

PIROXICAM -NSAIDs Antipyretics-Analgesics Drug

                                                               PIROXICAM                                   

MECHANISM OF ACTION-
 It involves inhibition of cyclooxygenase ( COX-1 and COX-2). Piroxicam is a potent inhibitor of prostaglandin synthesis in vitro.

USES-
1. Anti-inflammatory in rheumatoid
2. Acute gout
3. Musculoskeletal injuries
4. dentistry

SIDE EFFECTS-
1. Faecal blood loss
2. Rashes
3. Pruritus
4. Edema

PHARMACOLOGICAL  ACTION-
It has analgesic, and antipyretic properties.

DRUG-DRUG INTERACTION-
Piroxicam + Aliskiren = decreases antihypertensive adtivity of aliskiren.
Piroxicam + Citric acid = increase anticoagulant activity.
Piroxicam + Diclofenac = increase risk of adverse effect.

REFERENCE : Tripathi K.D ; ''Essentials Of Medical Pharmacology' ;Seventh edition; Page no. 192,201-202,208,213

PIRENZEPINE - DRUG ACTING ON ANS

                                                         PIRENZEPINE
                                                                                              
MECHANISM OF ACTION- 
It is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The Muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G protein.

USES- 
1. Antisecretory action
2. Peptic ulcer
3. Antispasmodic
4. Bronchial asthama
5. Mydriatic

SIDE EFFECTS-
1. Dry mouth
2. Rashes
3. Fever
4. Photophobia
5. Blurred vision

PHARMACOLOGICAL  ACTION-
It stimulates medullary centre.
It produces tachycardia.
Visceral smooth muscles are relaxed.
Decreases sweat , salivary or tracheobronchial secretion.

DRUG-DRUG INTERACTION- 
Cimetidine + Pirenzipine = lowers gastric secretion

REFERENCE : Tripathi KD ;Essentials of medical pharmacology; seventh edition; page no. 101,115,117,654

PIOGLITAZONE-ORAL HYPOGLYCEMICS DRUG

                                                                                                                                                                                                                                  PIOGLITAZONE

MECHANISM OF ACTION-
 It tends reverse insulin resistance by enhancing GLUT4 expression and translocation.

USES-
1. Oral anti-daiabetic
2. Lowers serum triglyceraldehyde level
3. Increases HDL
SIDE EFFECTS-
1. Plasma vo
 lume expansion
2. Edema
3. Weight gain
4. Headache
5. Mild anaemia

PHARMACOLOGICAL ACTION-
It reduces blood glucose and HbA1c without increasing circulating insulin.
It is used as a supplement to SUD/Metformin.

DRUG-DRUG INTERACTION-
Pioglitazone + Rifampin = induce metabolism of pioglitazone
Pioglitazone + Ketoconazole = inhibit metabolism of pioglitazone

Reference-Tripathi KD," Essentials of Medical Pharmacology", 7th edition, page no-270,272,276-277,279,280

PINDOLOL-ANTIADERNERGIC DRUG : SIDE EFFECT AND USES

                                                  PINDOLOL

INTRODUCTION-
It has been used primarily as antihypertensive : may be advantages in patients who develop marked bardycardia with propanolol. chances rebound  hypertension on withdrawal are also less.

MECHANISM OF ACTION-
 Pindolol non-selectively blocks ß-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure.

USES-
1. Antihypertensive
2. High blood pressure
3. Heart attack
4. Kidney problem

SIDE EFFECTS-
1. Chest pain
2. Heart attack
3. Irregular heartbeat

PHARMACOLOGICAL  ACTION-
Pindolol is a nonselective ß blocker with partial ß adrenergic receptor agonist activity and also possesses intrinsic sympathomimetic activity.
It also shows membrane stabiling effects .

DRUG-DRUG INTERACTION-
Pindolol + Heptabarbital = decrease the serum concentration of ß-blockers
Pindolol + Amiodarone = may enhance the bradycardic effect of ß-blockers.

REFERENCE-
 ESSENTIAL OF MEDICAL PHARMACOLOGY BY K.D TRIPATHI 7th edition pg. no.-144,147

PILOCARPINE -CHOLINERGIC DRUG :SIDE EFFECT AND USES

                                                                       PILOCARPINE 

INTRODUCTION                                                  

Pilocarpine is a choline ester miotic and a positively charged quaternary ammonium compound. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of pilocarpine.

MECHANISM OF ACTION

Pilocarpine is a cholinergic parasympathomimetic agent. It increase secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.

USES

For the treatment of radiation-induced dry mouth (xerostomia) and symptoms of dry mouth in patients with Sjögrens syndrome.
used as a miotic and in the treatment of glaucoma

SIDE EFFECT

•shortness of breath;
•fast or slow heart rate;
•severe headache, pounding in your neck or ears;
•confusion, tremors; or
•a light-headed feeling, like you might pass out.
Common side effects may include:
•increased sweating, urinating more than usual;
•chills, or flushing (warmth, redness, or tingly feeling);
•headache, dizziness, weakness;
•nausea, vomiting, diarrhea;
•blurred vision, watery eyes; or
•runny nose.

DRUG DRUG INTERACTION

Cimetropium Bromide
Pilocarpine may decrease the anticholinergic activities of Cimetropium Bromide.
Nadolol
The risk or severity of adverse effects can be increased when Nadolol is combined with Pilocarpine.
Tacrine
The risk or severity of adverse effects can be increased when Tacrine is combined with Pilocarpine.
       REFERENCE-
 ESSENTIAL OF MEDICAL PHARMACOLOGY BY K.D TRIPATHI 7th edition pg.no.-102, 103                                               
                                                               

PHYSOSTIGMINE -CHOLINERGIC DRUG:SIDE EFFECT AND USES

                                              PHYSOSTIGMINE-   

INTRODUCTION

Physostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor which effectively increases the concentration of acetylcholine at the sites of cholinergic transmission. Physostigmine is used to treat glaucoma. Because it crosses the blood-brain barrier, it is also used to treat the central nervous system effects of atropine overdose and other anticholinergic drug overdoses. Physostigmine can reverse both central and peripheral anticholinergia

MECHANISM OF ACTION

Physostigmine inhibits acetylcholinesterase, the enzyme responsible for the breakdown of used acetylcholine. By interfering with the metabolism of acetylcholine, physostigmine indirectly stimulates both nicotinic and muscarinic receptors due to the consequential increase in available acetylcholine at the synapse.

USES

used to treat glaucoma and delayed gastric emptying
used to treat anticholinergic poisoning .
used to reverse neuromuscular blocking.

SIDE EFFECT

overdose can cause cholinergic syndrome
nausea,
 vomiting,
diarrhea,
anorexia,
dizziness,
 headache,
 stomach pain,
sweating,
 dyspepsia,
 seizures

DRUG INTERACTION

Acetylcholine
The risk or severity of adverse effects can be increased when Physostigmine is combined with Acetylcholine.
Atracurium besylate
Physostigmine may decrease the neuromuscular blocking activities of Atracurium besylate.
Carbachol
The risk or severity of adverse effects can be increased when Physostigmine is combined with Carbachol.
Dipyridamole
The therapeutic efficacy of Physostigmine can be decreased when used in combination with Dipyridamole.
Fludrocortisone
The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Physostigmine.
Nadolol
Physostigmine may increase the bradycardic activities of Nadolol.
Procyclidine
The therapeutic efficacy of Procyclidine can be decreased when used in combination with Physostigmine.
Succinylchol
The serum concentration of Succinylcholine can be increased when it is combined with Physostigmine.
 REFERENCE-
 ESSENTIAL OF MEDICAL PHARMACOLOGY BY K.D TRIPATHI7th edition pg.no.105-110
                                                                   

PHOLCODINE - ANTITUSSIVE DRUG : SIDE EFFECT AND USES

                                                 PHOLCODEINE

INTRODUCTION

Pholcodine is a drug which is an opioid cough suppressant (antitussive). It helps suppress unproductive coughs and also has a mild sedative effect, but has little or no analgesic effects. It is also known as morpholinylethylmorphine and homocodeine. Pholcodine is not prescribed in the United States where it is classed as a Schedule I drug

USES

Use as cough suppresent.

MECHANISM OF ACTION

Pholcodine is readily absorbed from the gastrointestinal tract and freely crosses the blood–brain barrier. It acts primarily on the central nervous system (CNS), causing depression of the cough reflex, partly by a direct effect on the cough centre in the medulla. It is metabolized in the liver and its action may be prolonged in individuals with hepatic insufficiency (i.e. liver problems). Its use is therefore contraindicated in patients with liver disease, while care is advised in patients with hepatic impairment

SIDE EFFECTS

dizziness
 gastrointestinal disturbances such as nausea or vomiting.
 Adverse effects such as constipation, drowsiness, excitation, ataxia and respiratory depression have been reported occasionally or after large doses.
REFERENCE-
 ESSENTIAL OF MEDICAL PHARMACOLOGY BY K.D TRIPATHI7th edition pg. no. 220,474

PHENYTOIN -ANTIEPILEPTIC:SIDE EFFECT AND USES

                                                PHENYTOIN                      

Phenytoin is an antiepileptic drug which can be useful in the treatment of epilepsy. The primary site of action appears to be the motor cortex where spread of seizure activity is inhibited. Phenytoin reduces the maximal activity of brain stem centers responsible for the tonic phase of tonic-clonic (grand mal) seizures. Phenytoin acts to dampen the unwanted, runaway brain activity seen in seizure by reducing electrical conductance among brain cells. It lacks the sedation effects associated with phenobarbital. There are some indications that phenytoin has other effects, including anxiety control and mood stabilization, although it has never been approved for those purposes by the FDA. Phenytoin is primarily metabolized by CYP2C9.

MECHANISM OF ACTION

Phenytoin acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. By promoting sodium efflux from neurons, phenytoin tends to stabilize the threshold against hyperexcitability caused by excessive stimulation or environmental changes capable of reducing membrane sodium gradient. This includes the reduction of post-tetanic potentiation at synapses. Loss of post-tetanic potentiation prevents cortical seizure foci from detonating adjacent cortical areas.

SIDE EFFECT

hives;

difficulty breathing;

_swelling of your face, lips, tongue, or throat. fever, swollen glands, sore throat, trouble breathing, painful mouth sores, sores around your eyes;

•skin rash, easy bruising or bleeding, severe weakness;

•severe muscle pain;

•nausea, vomiting, upper stomach pain, loss of appetite, dark urine, jaundice (yellowing of the skin or eyes);

•bone pain (especially in your hips, legs, or lower back), trouble with walking; or

•severe skin reaction--fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Common phenytoin side effects may include:

•nausea, vomiting, constipation;

•tremors, slurred speech, loss of balance or coordination;

•rash;

•headache;

•confusion, dizziness, nervousness; or

•sleep problems (insomnia).

swelling of your face, lips, tongue, or throat.

USES           

used to control seizures

DRUG DRUG INTERACTION

Abiraterone

The serum concentration of Abiraterone can be decreased when it is combined with Phenytoin.

Acenocoumarol

Phenytoin may increase the anticoagulant activities of Acenocoumarol.

Acetaminophen

The serum concentration of Acetaminophen can be decreased when it is combined with Phenytoin.

Acetazolamide

The risk or severity of adverse effects can be increased when Acetazolamide is combined with Phenytoin.

Afatinib

The serum concentration of Afatinib can be decreased when it is combined with Phenytoin.

Albendazole

The serum concentration of the active metabolites of Albendazole can be reduced when Albendazole is used in combination with Phenytoin resulting in a loss in efficacy.

Alfuzosin

The metabolism of Alfuzosin can be increased when combined with Phenytoin.

Alprazolam

The serum concentration of Phenytoin can be increased when it is combined with Alprazolam.

Aminophylline

The serum concentration of Aminophylline can be decreased when it is combined with Phenytoin.

Amiodarone

The serum concentration of Amiodarone can be decreased when it is combined with Phenytoin.

REFERENCE-

 ESSENTIAL OF MEDICAL PHARMACOLOGY BY K.D TRIPATHI7th edition pg.no.-412-422

                                                                       

                                                                        

PHENYLEPHRINE - ALPHA 1 RECEPTOR SELECTIVE ANTAGONIST : ITS SIDE EFFECTS AND USES

INTRODUCTION-

Phenylephrine is a sympathomimetic amine that acts predominantly on a-adrenergic receptors. It is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs.

MECHANISM OF ACTION-

In general, a1-adrenergic receptors mediate contraction and hypertrophic growth of smooth muscle cells. a1-receptors are 7-transmembrane domain receptors coupled to G proteins, Gq/11. Three a1-receptor subtypes, which share approximately 75% homology in their transmembrane domains, have been identified: a1A (chromosome 8), a1B (chromosome 5), and a1D (chromosome 20). Phenylephrine appears to act similarly on all three receptor subtypes. All three receptor subtypes appear to be involved in maintaining vascular tone. The a1A-receptor maintains basal vascular tone while the a1B-receptor mediates the vasocontrictory effects of exogenous a1-agonists. Activation of the a1-receptor activates Gq-proteins, which results in intracellular stimulation of phospholipases C, A2, and D. This results in mobilization of Ca2+ from intracellular stores, activation of mitogen-activated kinase and PI3 kinase pathways and subsequent vasoconstriction. Phenylephrine produces its local and systemic actions by acting on a1-adrenergic receptors peripheral vascular smooth muscle. Stimulation of the a1-adrenergic receptors results in contraction arteriolar smooth muscle in the periphery. Phenylephrine decreases nasal congestion by acting on a1-adrenergic receptors in the arterioles of the nasal mucosa to produce constriction; this leads to decreased edema and increased drainage of the sinus cavities

USES-

used for the temporary relief of stuffy nose, sinus, and ear symptoms caused by the common cold, flu, allergies, or other breathing illnesses (e.g., sinusitis, bronchitis).

SIDE EFFECT-

1-Mild upset stomach

2- trouble sleeping

3- dizziness

4- lightheadedness

5- headache

6- nervousness

7- shaking or fast heartbeat may occur.

DRUG DRUG INTERACTION-

1-Acebutolol

The risk or severity of adverse effects can be increased when Acebutolol is combined with Phenylephrine.

2-Acetaminophen

The serum concentration of Phenylephrine can be increased when it is combined with Acetaminophen.

3-Acetylsalicylic acid

The risk or severity of adverse effects can be increased when Phenylephrine is combined with Acetylsalicylic acid.

4-Alfuzosin

Alfuzosin may decrease the vasoconstricting activities of Phenylephrine.

5-Aminophylline

The risk or severity of adverse effects can be increased when Phenylephrine is combined with Aminophylline.

6-Amitriptyline

Amitriptyline may increase the activities of Phenylephrine.

7-Amphetamine

The risk or severity of adverse effects can be increased when Phenylephrine is combined with Amphetamine.

8-Arformoterol

The risk or severity of adverse effects can be increased when Phenylephrine is combined with Arformoterol.

9-Armodafinil

The risk or severity of adverse effects can be increased when Phenylephrine is combined with Armodafinil.

10-Articaine

The risk or severity of adverse effects can be increased when Phenylephrine is combined with               Articaine.                                                                                                 

                                                                                                                  

REFERENCE-

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.127                                                                   

                                                                           

                                                                                                                   

PHENYLBUTAZONE - PYRAZOLONE DERIVATIVE : ITS SIDE EFFECTS AND USES

INTRODUCTION-

Phenylbutazone is a synthetic, pyrazolone derivative. It is a nonhormonal anti-inflammatory, antipyretic compound useful in the management of inflammatory conditions. The apparent analgesic effect is probably related mainly to the compound's anti-inflammatory properties and arise from its ability to reduce production of prostaglandin H and prostacyclin. Prostaglandins act on a variety of cells such as vascular smooth muscle cells causing constriction or dilation, on platelets causing aggregation or disaggregation and on spinal neurons causing pain. Prostacylcin causes vascular constriction platelet disaggregationPhenylbutazone, often referred to as "bute",[1] is a nonsteroidal anti-inflammatory drug (NSAID) for the short-term treatment of pain and fever in animals.
In the United States and United Kingdom, it is no longer approved for human use, as it can cause severe adverse effects such as suppression of white blood cell production and aplastic anemia

MECHANISM OF ACTION-

Phenylbutazone binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.

USES-

1-use in humans for the treatment of rheumatoid arthritis and gout
2-used to treat ankylosing spondylitis, but only when other therapies are unsuitable in UK

SIDE EFFECT-

1-gastrointestinal ulcers,
2-blood dyscrasia,
3- kidney damageoral lesions if given by mouth,


DRUG DRUG INTERACTION-

Phenylbutazone may affect blood levels and duration of action of phenytoin, valproic acid, sulfonamides, sulfonylurea antidiabetic agents, barbiturates, promethazine, rifampicin, chlorpheniramine, diphenhydramine, and penicillin G.

REFERENCE-                                                                     
 
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.192                                                                       
                                                                             

PHENOL - CAUSTICS AND ESCHAROTICS : ITS SIDE EFFECTS AND USES

INTRODUCTION-

Phenol is an antiseptic and disinfectant. It is active against a wide range of micro-organisms including some fungi and viruses, but is only slowly effective against spores. Phenol has been used to disinfect skin and to relieve itching. Phenol is also used as an oral analgesic or anesthetic in products such as Chloraseptic to treat pharyngitis. Research indicates that parental exposure to phenol and its related compounds are positively associated with spontaneous abortion. During the second world war, phenol injections were used as a means of execution by the Nazis. Phenol is a toxic compound whose vapours are corrosive to the skin, eyes, and respiratory tract.

MECHANISM OF ACTION-

Phenol is a potent proteolytic agent. Concentrations in the 5% to 7% range dissolve tissue on contact via proteolysis. In high concentrations when injected next to a nerve, phenol produces a chemical neurolysis which is nonselective across nerve fiber size and most prominent on its outer aspect. Local anesthetic effects occur within 5-10 minutes.

USES-

1-Used in treatment of focal spasticity
2-Used for minor sore throat pain, sore mouth, minor mouth irritation, and pain associated with canker sore.
3- Phenol is also used as an oral anesthetic/analgesic.

SIDE EFFECT-

 1-dermatitis,
2- lung edema.
3-dysrhythmia,
4-seizures,
5- coma.
                                                                                                                                                                    REFERENCE-                                     
                                                                                                     

 Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.889

PHENIRAMINE - H1 ANTIHISTAMINICS (MODERATELY SEDATIVE) : ITS SIDE EFFECTS AND USES

INTRODUCTION-

Pheniramine is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It has relatively strong sedative effects, and may sometimes be used off-label as an over-the-counter sleeping pill in a similar manner to other sedating antihistamines such as diphenhydramine. Pheniramine is also commonly found in eyedrops used for the treatment of allergic conjunctivitis.
Pheniramine is generally sold in combination with other medications, rather than as a stand-alone drug, although some formulations are available containing pheniramine by itself. As an example, Neo Citran contains pheniramine.

USES-

1-Used to temporarily relieve symptoms caused by the common cold, flu, allergies, or other breathing illnesses (such as sinusitis, bronchitis).
2-It help to relieve watery eyes, itchy eyes/nose/throat, runny nose, and sneezing.

SIDE EFFECTS-

1- Drowsiness or bradycardia,
2-Over-dosage may lead to sleep disorders
3- Seizures
4-Loss of consciousness.

MECHANISM OF ACTION-

Antihistamines such as pheniramine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release. Antihistamines suppress the histamine-induced wheal (swelling) and flare (vasodilation) response by blocking the binding of histamine to its receptors on nerves, vascular smooth muscle, glandular cells, endothelium, and mast cells. They effectively exert competitive antagonism of histamine for H1-receptors.


DRUG DRUG INTERACTION-
1-Acebutolol
The risk or severity of adverse effects can be increased when Acebutolol is combined with 2-Pheniramine.
2-Alfuzosin
Alfuzosin may decrease the vasoconstricting activities of Pheniramine.
3-Amitriptyline
Amitriptyline may increase the activities of Pheniramine.
4-Amphetamine
The risk or severity of adverse effects can be increased when Amphetamine is combined with Pheniramine.
5-Benzphetamine
The risk or severity of adverse effects can be increased when Benzphetamine is combined with 6-6-Pheniramine.
6-Cabergoline
Cabergoline may increase the hypertensive activities of Pheniramine.
7-Chlorphentermine
The risk or severity of adverse effects can be increased when Chlorphentermine is combined with Pheniramine.
.
8-Dobutamine
The risk or severity of adverse effects can be increased when Dobutamine is combined with Pheniramine.
9-Dopamine
The risk or severity of adverse effects can be increased when Dopamine is combined with Pheniramine.

REFERENCE-
                                                                       
 Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.164                                                                     
                                                      

PHENCYCLIDINE - ARYLCYCLOHEXYL AMINES :ITS SIDE EFFECTS AND USES

INTRODUCTION-

Phencyclidine (PCP), also known as angel dust and Sernyl among others, is a dissociative drug. PCP was brought to market in the 1950s as an anesthetic pharmaceutical drug but was taken off the market in 1965 due to the high prevalence of dissociative hallucinogenic side effects. PCP is a member of the arylcyclohexylamine class, and, in pharmacology, it is a member of the family of dissociative anesthetics. PCP works primarily as an NMDA receptor antagonist, where it blocks the activity of the NMDA receptor. As an addictive drug, PCP is associated with compulsive abuse

MECHANISM OF ACTION-

The N-methyl-D-Aspartate (NMDA) receptor, a type of ionotropic receptor, is found on the dendrites of neurons and receives signals in the form of neurotransmitters. It is a major excitatory receptor in the brain. Normal physiological function requires that the activated receptor fluxes positive ions through the channel part of the receptor. PCP enters the ion channel from the outside of the neuron and binds, reversibly, to a site in the channel pore, blocking the flux of positive ions into the cell. PCP therefore inhibits depolarization of neurons and interferes with cognitive and other functions of the nervous system

USES-

Used as a pesticide and a disinfectant.

SIDE EFFECTS-

1-Unsteady gait
2-Slurred speech
3-Bloodshot eyes
4-Loss of balance

REFERENCE-

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.452                                                                 
                                                                 

PROBENECID - ORGANIC ACID TRANSPORT : ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION –

 Probencid  inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Probencid may also reduce plasma binding of urate and inhibit renal secretion of uric acid at subtherapeutic concentrations. The mechanism by which probencid inhibits renal tubular transport is known, but the drug may inhibit transport enzymes that require a source of high energy phosphate bonds and/or nonspecifically interefere with substrate access to peotein receptor sites on the kidney tubules.

PHARMACOLOGICAL ACTION –

1- The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate.
2- Probencid has also been used to treat patients with renal impairment , and , because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.

USES –

1. Probencid  is primarily used to treat gout amd hyperuricemia.
2. It is sometime used to increase the concentration of some antibiotics.
3. It has also found use as a masking agent .

SIDE EFFECTS –

1-Nausea, vomiting , headache.
2-Lower back pain
3- Painful urination , frequent urination
4-Loss of apetite
5-Dizziness
6-Sore gums

DRUG-DRUG INTERACTION –

1-Probencid + Aspirin = therapeutic efficacy of probencid can be decreased when used in combination with Aspirin.
2-Probencid + Amoxicillin = the serum concentration of Amoxicillin can be increased when it is combined with Probencid.

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.30

PREGABALIN - ANTIEPILEPTIC DRUG CYCLIC GABA ANALOUGES : ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION –

 Pregabalin binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. Although the mechanism of action of pregabalin is unknown, results with genetically modified mice and with compounds structurally related to pregabalin (such as gabapentin) suggest that binding to the alpha2-delta subunit may be involved in pregabalin's antinociceptive and antiseizure effects in animal models. In vitro, pregabalin reduces the calcium-dependent release of several neurotransmitters, possibly by modulation of calcium channel function. Studies also suggest that the descending noradrenergic and serotonergic pathways originating from the brainstem may be involved with the mechanism of pregabalin. Interestingly, although pregabalin is a structural derivative of inhibitory neurotransmitter gamma-aminobutyric acid (GABA), it does not bind directly to GABA or benzodiazepine receptors. The sodium channels, opiate receptors, and cyclooxygenase enzymes are not involved with the mechanism of pregabalin. It is also inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake.

PHARMACOLOGICAL ACTION –

1-Pregabalin binds to the alpha2-delta subunit of the voltage-gated calcium channel in the central nervous system.
2- While pregabalin is a structural derivative of the inhibitory neurotransmitter gamma- aminobutyric acid (GABA), it does not bind directly to GABA-A, GABA-B, or benzodiazepine receptors, does not augment GABA-A responses in cultured neurons, does not alter rat brain GABA concentration or have acute effects on GABA uptake or degradation.
3-However, in cultured neurons prolonged application of pregabalin increases the density of GABA transporter protein and increases the rate of functional GABA transport.
4-Pregabalin does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity.
5- It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake.

USES –

1. It is used to treat pain caused by nerve damage due to diabetes or to shingles (herpes zoster) infection.
2. It may also be used to treat nerve pain caused by spinal cord injury.
3. This is also used to treat pain in people with fibromyalgia.
4. It is also used with other medications to treat certain types of seizures.

SIDE EFFECTS –

1-Drowsiness
2-Dizziness
3-Dry mouth
4-Constipation
5-Swollen arms
6-Weight gain.

DRUG-DRUG INTERACTION –

1-Pregabalin + Azelastine = may increase the CNS depressant activity of Azelastine.
2-Pregabalin + Captopril = risk or severity of adverse effect can be increase.
3-Pregabalin + Benazapril = risk or severity of adverse effect can be increase.

REFERENCE-

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.419

PREDNISOLONE - CORTICOSTEROIDS : ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION –

 As a synthetic glucocorticoid (GC), its lipophilic structure allows for easy passage through the cell membrane where it then binds to its respectively glucocorticoid receptor (GCR) located in the cytoplasm. Upon binding, formation of the GC/GCR complex causes dissociation of chaperone protein from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus. This process occurs within 20 minutes of binding. Once inside the nucleus,the homodimer GC/GCR complex binds to specific DNA binding-sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to synthesis of anti-inflammatory proteins while binding to negative GREs block the transcription of inflammatory genes.

PHARMACOLOGICAL ACTION –

1-Inhibit glucose utilization by peripheral tissue.
2-Promote lipolysis.
3-Enhance renal excretion of calcium.
4-Secretion of gastric acid and pepsin is increased.

USES –

1. Acute adrenal insufficiency.
2. Addison’s disease
3. Congenital adrenal hyperplasia
4. Arthritis
5. Autoimmune diseases
6. Bronchial asthma
7. Cerebral edema.

SIDE EFFECTS –

1-Increase appetite, weight gain, nausea
2-Increase risk of infection
3-Cardiovascular events in children
4-Dermatological effects including reddening of face, bruising/ skin discoloration, impaired wound healing, thinning of skin, skin rash, fluid build up and abnormal hair growth.
5-Menstrual abnormalities
6-Less response to hormones especially during stressful instances such as surgery or illness.
7-Change in electrolytes: rise in BP, increase sodium and low potassium leading to alkalosis.
8-GI system effects: Swelling of stomach lining, reversible increase in liver enzymes and risk of stomach ulcer
9-Muscular and skeletal abnormalities such as muscle weakness and loss, osteoporosis, long bone fractures, tendon rupture and back fractures.

DRUG-DRUG INTERACTION –

1-Prednisolone + moxifloxacin = can increase the risk of tendinitis and tendon rupture.
2-Prednisolne + Bupropion = may increases the chances of seizures.

REFERENCE-

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.230

PRAZOSIN- SELECTIVE ANTAGONIST ITS SIDE EFFECT AND USES

MECHANISM OF ACTION –

 Prazosin acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation.

PHARMACOLOGICAL ACTION –

1- Prazosin is a selective inhibitor of the alpha1 subtype of alpha adrenergic receptors.
2- In the human prostate, Prazosin antagonizes phenylephrine (alpha1 agonist)-induced contractions, in vitro and binds with high affinity to the alpha1c adrenoreceptor, which is thought to be the predominant functional type in the prostate.
3- The antihypertensive effect of Prazosin results from a decrease in systemic vascular resistance and the parent compound Prazosin is primarily responsible for the antihypertensive activity.

USES –

1. Used to treat hypertension.
2. It has also been used to decrease urinary obstruction and relieve symptoms associated with symptomatic benign prostatic hyperplasia. a1-Receptors mediate contraction and hypertrophic growth of smooth muscle cells. Antagonism of these receptors leads to smooth muscle relaxation in the peripheral vasculature and prostate gland.
3. Prazosin has also been used in conjunction with cardiac glycosides and diuretics in the management of severe congestive heart failure.
4. It has also been used alone or in combination with ß-blockers in the preoperative management of signs and symptoms of pheochromocytoma.


SIDE EFFECTS –

1-Dizziness or lightheadednessfainting (sudden)
2-Loss of bladder control
3-pounding heartbeat
4-swelling of the feet or lower legs
5-Chest pain
6-trouble breathing

DRUG-DRUG INTERACTION –

1-Prazosin + Acebutolol = may increase the orthostatic hypotensive activities of Prazosin.
2-Prazosin +Alfuzosin = may increase the antihypertensive activities of Alfuzosin.
3-Prazosin + Atenolol = may increase the orthostatic hypotensive activities of Prazosin.

REFERENCE- 

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.127

PRAMIPEXOLE BRAIN DOPAMINERGIC AGONIST ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION –

Pramipexole acts on dopaminergic receptors.

PHARMACOLOGICAL ACTION –

1-Improvement occurs in parkinsonian patients.
2-Postural hypotension.
3-Inhibit prolactin release.

USES –

1. Treating the signs and symptoms of Parkinson disease.
2. It is also used to treat restless legs syndrome (RLS).

SIDE EFFECTS –

1- Drowsiness
2- Hallucinations nausea
3- Trouble sleeping
4- Twitching, twisting, or other unusual body movements
5- Confusion
6- cough
7- difficulty with swallowing
8- double vision or other changes in vision
9- falling asleep without warning
10- fearfulness, suspiciousness, or other mental changes
11- fever
12- frequent urination
13- memory loss
14- muscle or joint pain
15- muscle weakness
16- restlessness or need to keep moving
17- swelling of the body
18- tightness in the chest


DRUG-DRUG INTERACTION –

Pramipexole + Propoxyphene = may increase side effects such as dizziness, drowsiness, confusion, and difficulty concentrating.

REFERENCE-

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.425

POSACONAZOLE SYSTEMIC MYCOSES ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION- 
It inhibits fungal CYP450 enzyme lanosterol  14- demethylase and thus impairs ergosterol synthesis leading to a cascade of membrane abnormalities in the fungus.

USES-
1. To treat infections by Candida , Aspergillus , or fusarium species.

SIDE EFFECTS-
1. Nausea
2. Abdominal pain
3. Loose motion
4. Headache
5. Dizziness
6. drowsiness

PHARMACOLOGICAL ACTION-
It blocks the synthesis of ergosterol.
It is significantly more potent at inhibiting 14-a demethylase than itraconazole.

DRUG-DRUG INTERACTION-
Posaconazole + H2 blocker = reduce gastric acidity
Posaconazole + phenytoin = decreases metabolism
Posaconazole + PPI = reduce gastric acidity

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.789

PIROXICAM NON- SELECTIVE COX INHIBITOR ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION-
 It involves inhibition of cyclooxygenase ( COX-1 and COX-2). Piroxicam is a potent inhibitor of prostaglandin synthesis in vitro.

USES-
1. Anti-inflammatory in rheumatoid
2. Acute gout
3. Musculoskeletal injuries
4. dentistry

SIDE EFFECTS-
1. Faecal blood loss
2. Rashes
3. Pruritus
4. Edema

PHARMACOLOGICAL  ACTION-
It has analgesic, and antipyretic properties.

DRUG-DRUG INTERACTION-
Piroxicam + Aliskiren = decreases antihypertensive adtivity of aliskiren.
Piroxicam + Citric acid = increase anticoagulant activity.
Piroxicam + Diclofenac = increase risk of adverse effect.

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no192

PIRENZIPINE SUBTYPYPE OF MUSCARINIC RECEPTOR ANTAGONIST ITS USES AND SIDE EFFECTS

MECHANISM OF ACTION- 
It is a muscarinic receptor antagonist and binds to the muscarinic acetylcholine receptor. The Muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G protein.

USES-
1. Antisecretory action
2. Peptic ulcer
3. Antispasmodic
4. Bronchial asthama
5. Mydriatic

SIDE EFFECTS-
1. Dry mouth
2. Rashes
3. Fever
4. Photophobia
5. Blurred vision

PHARMACOLOGICAL  ACTION-
It stimulates medullary centre.
It produces tachycardia.
Visceral smooth muscles are relaxed.
Decreases sweat , salivary or tracheobronchial secretion.

DRUG-DRUG INTERACTION- 
Cimetidine + Pirenzipine = lowers gastric secretion.

REFERENCE 

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.101

PIOGLITAZONE OVERCOME INSULIN RESISTANCE ITS USES AND SIDE EFFECTS

MECHANISM OF ACTION-

 It tends reverse insulin resistance by enhancing GLUT4 expression and translocation.

USES-

1. Oral anti-daiabetic

2. Lowers serum triglyceraldehyde level

3. Increases HDL

SIDE EFFECTS-

1. Plasma volume expansion

2. Edema 

3. Weight gain

4. Headache

5. Mild anaemia 

PHARMACOLOGICAL ACTION- 

It reduces blood glucose and HbA1c without increasing circulating insulin.

It is used as a supplement to SUD/Metformin.

DRUG-DRUG INTERACTION-

Pioglitazone + Rifampin = induce metabolism of pioglitazone

Pioglitazone + Ketoconazole = inhibit metabolism of pioglitazone

REFERENCE

 Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.270

PINDOLOL -I GENERATION BETA BLOCKER ITS SIDE EFFECTS AND USES

MECHANISM OF ACTION -

 Pindolol non-selectively blocks ß-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure.

USES-

1. Antihypertensive

2. High blood pressure

3. Heart attack

4. Kidney problem

SIDE EFFECTS-

1. Chest pain 

2. Heart attack

3. Irregular heartbeat

PHARMACOLOGICAL  ACTION-

Pindolol is a nonselective ß blocker with partial ß adrenergic receptor agonist activity and also possesses intrinsic sympathomimetic activity.

It also shows membrane stabiling effects .

DRUG-DRUG INTERACTION-

Pindolol + Heptabarbital = decrease the serum concentration of ß-blockers

Pindolol + Amiodarone = may enhance the bradycardic effect of ß-blockers. 

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.144

SULFSALAZINE DISEASE MODIFYING ANTI RHEUMATIC DRUG, DRUG FOR INFLAMMATORY BOWEL DISEASE, SPECIAL PURPOSE SULFONAMIDE AND IT'S PHARMACOLOGY

INTRODUCTION

A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid released in the colon.

 THERAPEUTIC USES

• To reduce inflammation and pain in rheumatism arthritis.
• Juvenile rheumatoid arthritis.
• Ulcerative colitis.

SIDE EFFECT

• Aching of joints
• Increased sensitivity of the skin to sunlight
• Fever
• Dark urine
• Bleeding gums
• Fast heartbeat
• Chest pain
• Bloody diarrhea

PHARMACOKINETICS

Bioavailability                                 <15%

Biological half-life                          5-10 hours

  

MECHANISM OF ACTION

In ulcerative colitis, clinical studies utilizing rectal administration of Sulfasalazine, SP and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety.

DRUG-DRUG INTERACTION

Sulfasalazine+Follic acid= The serum concentration of folic acid can be 

                                                 Decreased when it is combined with sulfasalazine.

Sulfasalazine+Mecamylamine= The risk of severity of adverse effects can be 

                                                      Increased when it is combine with mecamylamine.

Sulfasalazine+Methotrexate= It may increase the hepatotoxic activities of

                                                        Methotrexate.

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.210-211,683-684,706

SULFADIAZINE -SPECIAL PURPOSE SULFONAMIDES AND IT'S SIDE EFFECTS

INTRODUCTION

One of the short-acting sulfonamides used in combination with pyrimethamine to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infection.

 THERAPEUTIC USES

• In urinary tract infection
• Burns
• Toxoplasmosis

SIDE EFFECT

• Anxiety
• Blurred vision
• Coma
• Decrease sexual ability in males
• Depression
• Dizziness
• Fast heartbeat
• Feeling cold

MECHANISM OF ACTION

Sulfadiazine is a competitive inhibitor of the bacterial enzyme dihydropteoate synthetase. This enzyme is needed for the proper processing of para-aminobenzoic acid (PABA) which is essential for folic acid synthesis. The inhibited reaction is necessary in these organisms for the synthesis of folic acid.

DRUG-DRUG INTERACTION

Sulfadiazine+Alogliptin= It may increase the hypoglycemic activities of    

                                               Sulfadiazine.

Sulfadiazine+Bosentan= The serum concentration of bosentan can be increased

                                               When it is combined with sulfadiazine.

Sulfadiazine+Carvedilol= The serum concentration of carvedilol can be increased

                                                 When it is combined with sulfadiazine.            

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.704-705

SULFACETAMIDE - SPECIAL PURPOSE SULFONAMIDE AND ITS SIDE EFFECTS

Introduction

An anti-infective agent that is used topically to treat skin infections and orally for urinary tract infection.

  THERAPEUTIC USES

• Treating eye infection caused by certain bacteria
• Acne
• Seborrheic dermatitis

SIDE EFFECT

• Local/conjuctival irritation
• Stinging
• Burning
• Fungal corneal ulcers
• conjuctival hyperemia

PHARMACOKINETICS

Biological half-life                 7 to 12.8 hour

MECHANISM OF ACTION

Sulfacetamide is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), an essential component for bacterial growth. The inhibited reaction is necessary in these organisms for synthesis of folic acid.

Side effect

Sulfacetamide+Mecamylamine= The risk or severity of adverse effects can be 

                                                             Increased when sulfacetamide is combined 

                                                              With mecamylamine.

REFERENCE

Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.704-705