#pharmacology #newdrugs #lastlookrecentquestions #mustknow
Dr. Ajay Gupta
#pharmacology
#newdrugs
#lastlookrecentquestions
#mustknow

List of new drugs asked in last 2-3 year exams. HIGH YIELD LIST.

Anti HIV

COBICISTAT-    Pharmacokinetic enhancer. Cobicistat is a potent inhibitor of CYP3A4 subtype. Used with elvitegravir, an HIV integrase inhibitor. Additionally, with protease inhibitor darunavir and atazanavir  It also inhibits intestinal transport proteins, increasing the overall absorption of  atazanavir and darunavir.

Cancer Drugs

Ibrutinib is a small molecule drug that binds permanently to a protein, Bruton's tyrosine kinase (BTK), that is important in B cells; the drug is used to treat B cell cancers like mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenström's macroglobulinemia.

Crizotinib is a tyrosine kinase inhibitor. It works by blocking an enzyme called anaplastic lymphoma kinase (ALK). Crizotinib only works in cancer cells that have an overactive version of ALK. About 5%  with NSCLC ( Non Small Cell Lung Cancer)  have ALK positive disease. Anaplastic lymphoma kinase (ALK) positive Non Small Cell Lung Cancer

Ceritinib  and  Alectinib are also tyrosine kinase inhibitors used in ALK positive disease.

Tyrosine Kinase in CML ( Question on which is not a first line in CML)

Imatinib –First line
Dasatinib First line
Nilotinib  first line
Bosutinib –second line
Ponatinib –second line

Imatinib Side effects ( Question)

Common side effects can include diarrhea, nausea, muscle pain, and fatigue. Some people have itchy skin rashes.  Another common side effect is fluid build-up around the eyes, feet, or abdomen (belly). In rare cases the fluid may collect in the lungs or around the heart, which can cause trouble breathing. A person's white blood cell and platelet counts could possibly drop.

Other new cancer drugs which were asked in recent exams

Idelalisib is a second-line drug for patients whose chronic lymphocytic leukemia (CLL) has relapsed. The substance acts as a phosphoinositide 3-kinase inhibitor. 

Axicabtagene ciloleucel is a chimeric antigen receptor (CAR) T cell immunotherapy.  It consists of autologous T cells that are genetically modified to produce a CAR protein, allowing the T cells to identify and eliminate CD19-expressing normal and malignant cells. Approved in Diffuse large B-cell lymphoma (DLBCL).  Type of personalized immunotherapy. 

Rubidomycin Hydrochloride is another name of  Daunorubicin

Estramustine is a nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties. Estramustine is an Alkylating Drug.

Panitumumab is a fully human monoclonal antibody specific to the epidermal growth factor receptor approved for colorectal cancer.

ABRAXANE - Protein-bound paclitaxel, also known as nanoparticle albumin–bound paclitaxel or nab-paclitaxel, is an injectable formulation of paclitaxel used to treat breast cancer, lung cancer and pancreatic cancer, among others.

Aprepitant is an antiemetic drug  called substance P antagonists (SPA). It mediates its effect by blocking the neurokinin 1 (NK1) receptor.



Basiliximab is a chimeric mouse-human monoclonal antibody to the α chain (CD25) of the IL-2 receptor of T cells. It is used to prevent rejection in organ transplantation, especially in kidney transplants. ( CD 25 was the  question)


ALS

Edaravone is an intravenous medication used to help with recovery following a stroke  and to treat amyotrophic lateral sclerosis (ALS).   The drug is known to be an antioxidant, and oxidative stress has been hypothesized to be part of the process that kills neurons in people with ALS.

Side effects –include  hypersensitivity , bruising, gait disturbances, headache, skin inflammation, eczema, problems breathing, excess sugar in urine, and fungal skin infections.



Rheumatoid Arthitis 

Abatacept  regulates the activation of T cells by inhibiting the CD80/86:CD28 co-stimulatory pathway that is required for the proper T cell activation. Used in rheumatoid arthritis.  ( CD 28 was the question)

Tocilizumab, also known as  atlizumab, is an immunosuppressive drug, mainly for the treatment of rheumatoid arthritis (RA) and systemic juvenile idiopathic arthritis. It is a humanized monoclonal antibody against theinterleukin-6 receptor (IL-6R).

Oral Drugs -JAK STAT inhibitor

Tofacitinib, is a medication used to treat rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis. Common side effects include diarrhea, headache, and high blood pressure.

Baricitinib is similar drug .  Oral JAK STAT inhibitor

GIT Drugs 

Teduglutide  glucagon-like peptide-2 (GLP-2) analog that is used for the treatment of short bowel syndrome. It works by promoting mucosal growth and possibly restoring gastric emptying and secretion.

Racecadotril is an oral enkephalinase inhibitor for use in the treatment of acute secretary diarrhoea. By preventing the degradation of endogenous enkephalins, racecadotril reduces hypersecretion of water and electrolytes into the intestinal lumen.

Lubiprostone  is a chloride channel activator for oral use. It is used in the management of chronic idiopathic constipation, predominantly irritable bowel syndrome-associated constipation in women and opioid-induced constipation.

Renzapride is a gastroprokinetic agent and antiemetic which acts as a full 5-HT₄ full agonist and 5-HT₃ antagonist.

Melanosis coli is  seen with chronic use of Senna ( anthraquinones laxative).  The pigment deposition results in a characteristic dark brown to black discoloration of the lining of the large intestine. This condition is sometimes called pseudomelanosis coli because the pigment deposits consist of a pigment known as lipofuscin and do not contain melanin

IBD

Natalizumab is a humanized monoclonal antibody against the cell adhesion molecule α4-integrin. Natalizumab is used in the treatment of multiple sclerosis and Crohn's disease.

Vedolizumab  is a monoclonal antibody for the treatment of ulcerative colitis and Crohn's disease. It binds to integrin α4β7 (LPAM-1, lymphocyte Peyer's patch adhesion molecule 1).

Antibiotics

MDR Resistant Acinetobacter infection DOC -
COLISTMETHATE SODIUM ( Prodrug of Colistin) Side effect - Nephrotoxicity and Neurotoxicity



CARBAPENAMS – DOC for ESBL  (Question  was Longest acting Carbapenam )

Imipenem has the highest risk for seizure across the carbapenems *

Imipenem is broken down in the kidneys to a toxic metabolite by the DHP-1 enzyme Cilastatin* is  used to sustain the body’s levels of imipenem and prevent nephrotoxicity
Meropenem is the only carbapenem approved for MENINGITIS*

Ertapenem is LONGEST* acting administered every 24 hours. Rest all carbapenems every 6-8 hours. It lacks less activity against the P. aeruginosa and Acinetobacter species, both of which are important causes of hospital-acquired infections. LESS EFFECTIVE THEN OTHERS

Doripenem*.-  increases risk of death in patients with pneumonia. FDA ALERT

Topical Drugs for MRSA – Mupirocin, Fusidic acid, Retapumulin

CNS

PIMAVANSERIN-   Selective Antagonist of  serotonin 5-HT2A receptor. It is an atypical antipsychotic which is approved for the treatment of Parkinson's disease psychosis and for the treatment of schizophrenia.

Deutetrabenazine and

Valbenazine   Drugs approved for Tardive Kinesia

Retigabine  Voltage gated K channels , newer Antiepileptic for refractory partial seizure

Levetiracetam-  blocks N type Calcium Channels  Dose 30-40 mg/kg/day ( Dose was asked in question)

CVS

Vorapaxar

It is a reversible antagonist of the protease-activated receptor-1 (PAR-1) expressed on platelets. Vorapaxar inhibits thrombin- induced platelet aggregation but does not inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen or a thromboxane.

Vapiprost  a novel thromboxane receptor antagonist

Andexanet alfa ( Very important drug)

Xa reversal agent andexanet alfa quickly stopped the bleeding in patients who had an acut
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